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Aduri, Prakash Reddy* G. Suvarsha G. BabuRao T. Sudheer N. PhaniKumar. "FORMULATION AND INVITRO EVALUATION OF OXYBUTYNIN TRANSDERMAL PATCH." indo American Journal of Pharmaceutical Sciences 04, no. 05 (2017): 1398–405. https://doi.org/10.5281/zenodo.804920.
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The present study was aimed to develop transdermal drug delivery of Oxybutynin to overcome the first pass metabolism and to reduce frequency of dosing compared to oral route. Matrix type of transdermal patches was developed by using polymers eudragit L100 and eudragit S100.Transdermal patches were prepared by employing solvent casting method. Propylene glycol and Tween80 were selected as permeation enhancer and plasticizer. Drug excipient compatibility studies were carried out by using FTIR, and it was observed that there were no interactions. Formulations were prepared with the varying concentrations polymers ranging from F1-F9, and all the formulations were evaluated for various physical parameters Physical appearance, Flatness, Weight variation, Thickness, Folding endurance, Drug content, Moisture uptake, Moisture content and Swelling study and all the results were found to be were found to be with in the pharmacopeial limits, invitro drug release studies by using dialysis membrane. Among all the 12 formulations F6 formulation which contain HPMC K4M 300mg and Eudragit L-100 60mg had shown 94% cumulative drug release with in 12 hours. And compared to HPMC K15M, HPMC K4M showed better drug release profile. For F6 formulation release kinetics were plotted and the Regression coefficient value was found to be high for Korsmeyer-peppas release model i.e., 0.9892. The n value was found to be 0.6203 which indicates the drug release pattern was found to be non-Fickian diffusion. Key words: Oxybutynin, Matrix type, Transdermal patches.
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Wonglertnirant, Nanthida, S. Tipwichai, Praneet Opanasopit, Theerasak Rojanarata, Suwannee Panomsuk, and Tanasait Ngawhirunpat. "Development of Acrylic Matrix Type Ketoprofen Patch." Advanced Materials Research 506 (April 2012): 533–36. http://dx.doi.org/10.4028/www.scientific.net/amr.506.533.
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Ketoprofen transdermal patches (KTPs) were fabricated using an acrylic pressure sensitive adhesive (PSA) polymer. The influence of different factors (amount of PSA, drug content, and pressure applying on the backing membrane during preparation) on the characteristics of ketoprofen patch (thickness, W/A ratio, and adhesiveness of matrix film) and in vitro drug release behavior were investigated. The results revealed the successful fabrication and a good physical appearance of KTPs using acrylic PSA. Microscopic observations, FTIR spectra, and DSC thermograms were permitted to demonstrate that the drug was dispersed molecularly in the polymer. As the amount of PSA in the adhesive matrix was increased, the release rate of ketoprofen was decreased. Contrarily, the drug release rate was increased corresponding to the increase of ketoprofen content in the adhesive matrix. There was no significant difference in the release rate when the pressure applying on the backing membrane was varied. The kinetic of ketoprofen release from acrylic matrix type transdermal patches followed the Higuchis diffusion model.
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Hemangi, J. Patel, and S. Patel Jitendra. "Development of matrix type transdermal Patches of Tizanidine HCl." British Journal of Medical and Health Research 9, no. 11 (2022): 59–71. https://doi.org/10.5281/zenodo.7602506.
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Transdermal drug delivery system (TDDS) was designed to sustain the release and improve the bioavailability of drug and patient compliance. Among the various types of transdermal patches, matrix dispersion type systems disperse the drug in the solvent along with the polymers and solvent is allowed to evaporate forming a homogeneous drug-polymer matrix. Tizanidine Hydrochloride, an imidazoline derivative, is α2-adrenergic agonist and centrally acting myotonolytic skeletal muscle relaxant with a structure unrelated to other muscle relaxants. Tizanidine hydrochloride having lower bioavailability (40%) due to first pass metabolism by the liver. So, bioavailability can be increased by transdermal route. The object of the study was to develop Matrix Type Transdermal Patch of Tizanidine HCl. Transdermal patches were prepared by solvent evaporation method using Eudragit RS 100 and PVP polymers by incorporating Polyethylene Glycol and Propylene Glycol as plasticizer. Standard procedures were used to analyze the prepared films for various physicochemical parameters(weight variation, thickness uniformity, % moisture content, %moisture uptake, Folding Endurance and drug content). drug release (Franz diffusion cell) and skin irritation test. The drug and polymer compatibility was studied by DSC. Among all the formulations, the F1 prepared by using Eudragit RS 100 and PEG 400 as plasticizer is the better formulation for control release of drug up to 6 hrs of time. Results of the present study encouraged that the Tizanidine HCl with Eudragit RS 100 transdermal patch can be used as controlled drug delivery system and frequency of administration can be minimized. The kinetic models used were Zero order, First order Higuchi’s and Korsmeyer–Peppas model. Transdermal patches were successfully prepared for Tizanidine Hydrochloride and their evaluation suggested excellent quality and uniformity in patch characteristics. This can have potential applications in therapeutic area offering advantages in terms of reduced dosing frequency, improved patient compliance and bioavailability. Keywords: Tizanidine Hydrochloride, Eudragit RS 100, Matrix type, polyvinylpyrrolidone, Transdermal patches
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Saini, Mohit. "Release Kinetic Study of Matrix Type Transdermal Patch Using anAnalgesic Drug." IAR Journal of Medicine and Surgery Research 1, no. 1 (2020): 1–8. http://dx.doi.org/10.70818/iarjmsr.2020.v01i01.01.
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Transdermal therapeutic systems are defined as a self-contained, distinct dosage forms which, when applied to the intact skin, deliver the drug, through the skin at control rate to the systemic circulation. TDDS characterizes one of the most quickly advancing areas of novel drug delivery. TDDS are designed for controlled liberate of drug through the skin into systemic circulation maintaining consistent efficacy and reducing dose of the drug and its related side effects. Present study was conducted to prepare transdermal patch of Tramadol HCL with permeation enhancer to diminish extra side effects and to provide sustain drug delivery. Various kinetics models were examined for optimized formulation. The drug release data of all the formulation were fitted to different kinetic models to find out the kinetics of drug release from transdermal patch. The drug release data was also fitted to zero order (cumulative amount of drug release vs. time) power equation to find out the drug release mechanism.
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Priyanka, Priyanka, Rizwana Khan Rizwana Khan, and Bhawna Sharma Bhawna Sharma. "A Review on Transdermal Patch." International Journal of Pharmaceutical Research and Applications 10, no. 3 (2025): 518–29. https://doi.org/10.35629/4494-1003518529.
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Transdermal drug delivery (TDDS) is one of the most promising methods for drug application. Increasing numbers of drugs are being added to the list of therapeutic agents that can be delivered to the systemic circulation via the skin. Transdermal patch products were first approved by the FDA in 1981. Transdermal delivery is the most common painless technique of administering drugs to systemic circulation, providing controlled, constant administration of the drug, allowing continuous input of drugs with short biological half-lives, and eliminating pulsed entry into the systemic circulation. A transdermal patch is one such drug delivery technique, it is used to deliver a specific dose of drug through the skin into the systemic circulation. This review article summarizes the advantages of transdermal patches over conventional drug administration methods, some common components used in polymer matrix type patches, types of transdermal patches, factors affecting transdermal bioavailability, methods of preparation of transdermal patches, methods of evaluation, recent advancement, and some marketed formulations of transdermal patches. Thus, transdermal patches reduce the load that the oral route commonly places on the digestive tract and liver. It enhances patient compliance and minimizes the harmful side effects of a drug caused by temporary overdose.
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Suraj, B. Meshram, N. Dhembre* G., T. Jadhao U., T. Thoke S., A. Wathore S., and D. A. Rathod. "DEVELOPMENT AND EVALUATION OF TRANSDERMAL PATCH CONTAINING COLCHICINE." World Journal of Pharmaceutical Science and Research 3, no. 5 (2024): 182–91. https://doi.org/10.5281/zenodo.13870934.
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The present research work was intended to prepare transdermal patch containing Colchicine as a model drug. Matrix type of colchicine containing transdermal patch was prepared by solvent casting method using three rate controlling polymers like HPMCK4M, ethyl cellulose and PVPK30. Fixed concentration (2%) of all three polymers was utilized for the preparation of patch. Compatibility study of drug with the excipients was determined by I.R. Spectroscopy, Thickness of the patch was measured by using screw gauge. The thickness of prepared patch was found in the range of 0.310 to 0.315 mm. Batch F3 showed highest thickness of patch. The weight of the prepared transdermal patches for different formulations ranged between 52.14±1.20 to 55.70±1.98 mg. The percentage of drug content of formulation batch F1 to F7 varied between 94.04±1.23 to 97.26±0.31%.The folding endurance value for all batch formulations was found within range of 64 to 87. Patches formulated with ethyl cellulose (F2) showed the patch formulation F1, F2 and F3, formulated with HPMC, ethyl cellulose, and PVP K30, without addition of permeation enhancer in fixed concentration i.e. 2%, showed drug release of 72.16±0.33, 61.12±1.40 and 66.53±0.62% at the end of 24 hrs respectively. The developed optimized matrix type transdermal patch formulation was found to be stable during the stability study for the period of 3 month indicating good stability of the product.
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Suwannachote, Kongthong, and Garnpimol C. Ritthidej. "Development of Transdermal Patch Comprising Centella Asiatica Extract." Advanced Materials Research 93-94 (January 2010): 389–92. http://dx.doi.org/10.4028/www.scientific.net/amr.93-94.389.
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The purpose of this study was to develop matrix-type transdermal systems containing Centella asiatica extract for treatment of varicose veins by using various polymers such as ethylcellulose (EC), methylcellulose (MC), hydroxypropylmethylcellulose (HPMC), polyvinylpyrolidone (PVP) and hydroxyproply cellulose (HPC-H, HPC-M and HPC-L grades) at various concentrations (0.75%, 1.00%, 1.25%, 1.50%, 1.75% and 2.00%) and using 30% of propylene glycol (PG), diethyl phathalate (DEP), dibutyl phathalate (DBP), glycerine, polyethylene glycol (PEG) 400 as plasticizers. Centella asiatica extract at 7% of solid content of the formulation was added to the matrix formulation prior to pouring on backing layer which was prepared by using either EC as polymer and DBP as plasticizer or polyethylene wrap. It was found that the use of polyethylene wrap as backing layer, PG as plasticizer and HPC as matrix layer showed better appearance, flexibility and compatibility. It was also found that HPC-H and HPC-M showed high adhesion and stickiness. It was concluded that HPC at concentration of 1.75% and 2.00% could be formulated as satisfactory transdermal matrix-type patch for Centella asiatica extract.
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Bhumi, Patel* Dr. Chainesh Shah. "FABRICATION AND IN-VITRO CHARACTERIZATION OF TRANSDERMAL MATRIX PATCH OF KETOPROFEN FOR TRANSDERMAL THERAPEUTIC SYSTEM." Indo American Journal of Pharmaceutical Sciences (IAJPS) 03, no. 09 (2016): 960–73. https://doi.org/10.5281/zenodo.153859.
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Objective: The objective of research work was to improve the permeability of Ketoprofen and to provide controlled release of drug to provide maximum effective concentration. Experimental work: Transdermal drug delivery systems are polymeric patches containing dissolved or dispersed drugs that deliver therapeutic agents at a constant rate to the human skin. Matrix type transdermal patches containing Ketoprofen were prepared by solvent casting method employing aluminium foil method. Polyethylene glycol (PEG) 400 was used as plasticizer and Dimethyl sulfoxide (DMSO) was used as penetration enhancer. Polymers were selected on the basis of the their adhering and non-toxic property. Result and discussion Drug polymer interactions determine by FTIR and standard calibration curve of Ketoprofen were determine by using UV estimation. Transdermal patch was prepared by using HPMC K-4 M: PVP K-30, HPMC K-15 M: PVP K-30, HPMC K-100 M: PVP K-30, Eudragit RS-100:PVP K-30 showed good physical properties. All prepared formulations indicated good physical stability. In-vitro drug permeation studies of formulations were performed by using Franz diffusion cells using abdomen skin of Wistar albino rat. Result, showed best in-vitro skin permeation through rat skin (Wistar albino rat) as compared to all other formulations prepared with hydrophilic polymer containing permeation enhancer. The permeability of Ketoprofen was increased with increase in PVP content. The burst effect due to the incorporation of PVP was because of the rapid dissolution of the surface hydrophilic drug which gets swell and thus leads to the decrease of mean diffusional path length of the drug molecules to permeate into dissolution medium and higher permeation rates. Conclusion: It was observed that the formulation containing HPMC K-4 M: PVP K-30 (2:3) showed ideal higuchi release kinetics. Key words: Trasdermal drug delivery system, Polymers, Ketoprofen, Matrix type, Permiation
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Sharma, Aditya, and Navneet Verma. "Assessment of Analgesic and Anti-inflammatory Activity of Double-layered Diclofenac Diethylamine Transdermal Patch." Biomedical and Pharmacology Journal 15, no. 4 (2022): 1957–64. http://dx.doi.org/10.13005/bpj/2534.
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Diclofenac Diethylamine has been used generally in the management of pain and inflammation caused by musculoskeletal disorders. The current study revealed the preliminary investigation into the analgesic and anti-inflammatory activities of an optimized double-layered transdermal patch of Diclofenac Diethylamine. The patch was prepared by using the hydrophobic acrylic polymer Eudragit RL 100 and the hydrophilic polymer Polyvinyl pyrrolidone K-30 in combination as the first layer of matrix type and pressure-sensitive acrylic adhesive Duro Tak 387-2510 as the second layer of drug-in-adhesive type patch. The solvent casting method was employed to prepare the transdermal patch over the backing membrane. We optimized the patch in terms of its concentration based on results exhibited by ex-vivo and in-vitro studies using FDC and the rat’s skin. This study was designed to assess the analgesic and anti-inflammatory effects of an optimized patch with the respective models in laboratory animals. In a comparison of the developed transdermal patch with commercially available Diclofenac Diethylamine gel (Volini gel), the developed patch was found to be statistically significant (p < 0.01) and effective for decreasing pain and inflammation symptoms. The findings of the study suggest that the prepared double-layered transdermal patch of Diclofenac Diethylamine can serve as the best carrier to provide a sustained effect for the management of pain and inflammation.
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Fridayanti, Aditya, Esti Hendradi, and Isnaeni Isnaeni. "THE RELEASE OF SODIUM DICLOFENAC FROM MATRIX TYPE OF TRANSDERMAL PATCH." Journal Of Tropical Pharmacy And Chemistry 1, no. 2 (2011): 79–85. http://dx.doi.org/10.25026/jtpc.v1i2.13.
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Suksaeree, Jirapornchai, Akkharakunya Thuengernthong, Kanchala Pongpichayasiri, Pattwat Maneewattanapinyo, Sukanya Settharaksa, and Wiwat Pichayakorn. "Formulation and Evaluation of Matrix Type Transdermal Patch Containing Silver Nanoparticles." Journal of Polymers and the Environment 26, no. 12 (2018): 4369–75. http://dx.doi.org/10.1007/s10924-018-1305-5.
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Satya, Prakash Singh, Kumari Asha, and Kumar Sushil. "An Assessment of the Formulated Medicated Transdermal Patches Containing an Antidiabetic Drug: an in-Vitro Study." International Journal of Current Pharmaceutical Review and Research 15, no. 05 (2023): 529–36. https://doi.org/10.5281/zenodo.12627349.
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Conflict of interest: NilAbstractAim: The current research aims to formulate and evaluated medicated transdermal patchescontaining an antidiabetic drug.Material & Methods: In the present study was conducted by the Department ofPharmacology, DMCH, Laheriasarai, Darbhanga, Bihar, India. An attempt has been made todevelop a matrix-type transdermal therapeutic system comprising of various PVP K30, MCratios and solvent evaporation techniques. A good penetration enhancer would improve drugdelivery from various polymer-based transdermal patches. Transdermal patches of the matrixtype are made. All prepared formulations were tested for weight variation, thickness, drugcontent, moisture content, moisture uptake, flatness, and in vitro drug release. Bath F3 wasoptimised formula from all formulation baths shows linear zero order release for 24 hours,with a cumulative percentage of drug diffusion of 87.35% from 4cm2 patches. It has beendetermined that polymer concentration.Results: The formulated films were examined for colour, clearness, softness and elasticity. Itwas précised by digital Vernier calipers. Three reading were taken for standard deviationafter thickness measured at five various site of patch. The thickness of Glimepiride patcheswere between112.48-124.26μm. The folding endurance of patches was found to besatisfactory between 121.49±2.36 to 128.42±0.46. This shows that patches would maintaintheir integrity and not break easily. The moisture content in the patches was ranged from 1.38± 0.26 to 2.80 ± 0.20% (for formulation F series and formulation respectively). The weightvariation of Glimepiride patches were in between 250 to 280 mg. This showed uniformity inweight of patches while the % drug content of Glimepiride in patches were between 96.00 to95.15±0.85% this shows passable drug content in patches.Conclusion: When the concentration of PVP K30 increases in the primary layer, the in –vitro diffusion rate increases, and when the concentration of PVP K30 decreases, the drugdiffusion decreases. It allows for more controlled drug release from the patch.
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Senthil Kumar, K. L., P D Gokulan, A. Vasanthan, et al. "Preparation and evaluation of matrix type of transdermal patches containing anti –diabetic drug." Indian Journal of Pharmacy and Pharmacology 9, no. 1 (2022): 33–38. http://dx.doi.org/10.18231/j.ijpp.2022.006.
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The current research aims to formulate and evaluated medicated transdermal patches containing an anti-diabetic drug. A good penetration enhancer would improve drug delivery from various polymer-based transdermal patches. Transdermal patches of the matrix type are made. Using various PVP K30, MC ratios and solvent evaporation techniques. All prepared formulations were tested for weight variation, thickness, drug content, moisture content, moisture uptake, flatness, and in vitro drug release. Bath F3 was optimised formula from all formulation baths shows linear zero order release for 24 hours, with a cumulative percentage of drug diffusion of 87.35% from 4cm2 patches. It has been determined that polymer concentration. When the concentration of PVP K30 increases in the primary layer, the in – vitro diffusion rate increases, and when the concentration of PVP K30 decreases, the drug diffusion decreases. It allows for more controlled drug release from the patch.
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Posina Rakshitha, B. Deekshi Gladiola, and Cheepurupalli Prasad. "Formulation and biopharmaceutical evaluation of a transdermal patch containing letrozole." International Journal of Pharmaceuticals and Health Care Research 12, no. 4 (2024): 430–37. https://doi.org/10.61096/ijphr.v12.iss4.2024.430-437.
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The skin can be used as the site for drug administration for continuous transdermal drug infusion into the systemic circulation. For the continuous diffusion penetration of the drugs through the intact skin surface membrane-moderated systems, matrix dispersion type systems, adhesive diffusion controlled systems and micro reservoir systems have been developed. Various penetration enhancers are used for the drug diffusion through skin. In matrix dispersion type systems, the drug is dispersed in the solvent along with the polymers and solvent allowed to evaporate forming a homogeneous drug-polymer matrix. The results obtained showed no physical-chemical incompatibility between the drug and the polymers. L5 formulation has been selected as the best formulation among all the other formulations. The in-vitro drug diffusion studies from the formulation were found to be sustained release. All the evaluation parameters obtained from the best formulation were found to be satisfactory. The data obtained from the in-vitro release studies were fitted to various kinetic models like zero order, first order, Higuchi model and peppas model. From the kinetic data it was found that drug release follows Zero order kinetics model release by diffusion technique from the polymer.
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Shibanjan, Paul Roy-Guide Kamal Deka-Assistant Professor of Assam Royal Global University Shyam Prakash Rai-Sr.Lecturer of HGEA College of Pharmacy. "Role of a novel transdermal patch for both antihypertensive and antiparkinsonism activity." Pharma Innovation Journal 12, no. 4 (2023): 1150–57. https://doi.org/10.5281/zenodo.10036985.
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AbstractThe present invention is generally directed to matrix type transdermal patches for treating hypertension and Parkinson's disease. The present invention comprises of rasagiline mesylate and prazosin hydrochloride prepared by using different ratios of Eudragit RL 400 and hydoxy propyl methyl cellulose. Effect of protease granuleson permeation of rasagiline and prazosin analyzed. The patch so formed is nonirritant to the skin and possess maximum permeability. The present invention also relates to the method of producing the same. The transdermal patch shows 50% and 80% drug release for rasagiline mesylate and prazosin hydrochloride respectively in 250 hours. In this research total works done under the guidance of Guide-Mr. Shibanjan Paul Roy. Mr. Kamal Deka and Mr. Shyam Prakash Rai performed for the practical works and others work and note the reading.Keywords: Novel transdermal patch, both antihypertensive, antiparkinsonism activity
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Garude, Niket N., and Rachel B. Geevarghese. "Design and Characterization of Nanostructure Lipid Carrier for Transdermal Delivery of Pioglitazone." International Journal of Pharmaceutical Sciences and Nanotechnology 11, no. 4 (2018): 4185–95. http://dx.doi.org/10.37285/ijpsn.2018.11.4.6.
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Nanostructure Lipid Carrier (NLC) is one of the lipid-based drug delivery systems that are used as carrier for delivery of drugs. NLC are composed of mixture of solid lipid and liquid lipid, which form imperfect type of lipid matrix with improved drug loading capacity, drug release profile and stability. The aim of the present study was to develop and characterize nanostructure lipid carrier for transdermal delivery of pioglitazone (PZ) to overcome the problems related with oral route of administration and to improve systemic availability. NLC’s were prepared by high-speed homogenization method. Optimized NLC formulation was evaluated for particle size, percentage entrapment efficiency, surface morphology, DSC analysis, in-vitro drug release etc. The optimized NLC formulation was formulated as a transdermal patch and evaluated for in vitro drug release study and primary skin irritation study. In vivo hypoglycaemic activity of pioglitazone -NLC loaded transdermal patch was studied in comparison with its orally administered suspension. PZ- NLC loaded transdermal patch was found to be non-irritant and showed reduction in blood glucose level in a controlled manner up to 24 hrs.
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Linakis, Matthew W., Joseph E. Rower, Jessica K. Roberts, Eleanor I. Miller, Diana G. Wilkins, and Catherine M. T. Sherwin. "Population pharmacokinetic model of transdermal nicotine delivered from a matrix‐type patch." British Journal of Clinical Pharmacology 83, no. 12 (2017): 2709–17. http://dx.doi.org/10.1111/bcp.13393.
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Windriyati, Yulias Ninik, Risha Fillah Fithria, Fitria Dwi Kurniawati, and Ulfa Risalatul Mukaromah. "EVALUASI IN VITRO-IN VIVO FILM TRANDERMAL DILTIAZEM HCL DENGAN PENINGKAT PENETRASI PEG 400 SEBAGAI ANTIHIPERTENSI." JIFFK : Jurnal Ilmu Farmasi dan Farmasi Klinik 16, no. 01 (2019): 1. http://dx.doi.org/10.31942/jiffk.v16i01.2922.
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ABSTRACTDiltiazem HCL is an antihypertensive that low oral bioavailability of 40%, so developed to transdermal preparations. A matrix type of transdermal patch of diltiazem HCl was prepared using polyvinyl alcohol and ethyl cellulose with PEG 400 as penetration enhancer. In vitro-in vivo evaluation were conducted to asses drug permeation through the skin and determine the effectiveness of transdermal film as an antihypertensive drug. Transdermal patches of diltiazem HCl were evaluated for physicochemical characteristics weight variation, thickness, folding endurance, moisture uptake, and drug content. In vitro permeation study was conducted using commercial semi permeable membrane in Franz diffusion cell. In vivo activity study was evaluated on male rat Wistar that induced NaCl with CODA non-invasive blood pressure method. Transdermal patches of diltiazem HCl were found no significant differences in terms of physicochemical characteristics. The in vitro skin permeation profiles showed increased flux values with the increase of PEG 400 as a penetration enhancer. The in vivo evaluation showed a reduction in systolic and diastolic blood pressure within one hour after the drug administration. Diltiazem HCl was able penetration into skin, absorbed in blood circulation and effective as antihypertensive via transdermal route.Keywords : antihypertension, diltiazem HCl, PEG 400, transdermal patch
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Sharma, Aman, and Abhinav Agarwal. "FORMULATION AND EVALUATION OF TRANSDERMAL PATCH OF PLUMBAGIN FOR ANTI-FUNGAL ACTIVITIES." International Research Journal of Pharmacy 12, no. 2 (2021): 23–28. http://dx.doi.org/10.7897/2230-8407.1202122.
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The objective of the current study is to improve the patient compliance and sustained drug release action by herbal medicine which can be achieved by developing alternative drug delivery system. The matrix type transdermal patches containing plumbagin were prepared by solvent evaporation method with different ratios of polymers (HPMC 50cps, PVP K29-32 and EUDRAGIT RS-100). In these matrix type transdermal patches, the PEG (Polyethylene glycol) was used as plasticizer and DMSO (Dimethyl sulfoxide) used as a penetration enhancer. The formulated patches were evaluated for physicochemical parameters like thickness, weight variation, % moisture content, % moisture uptake, % flatness, folding endurance and drug content. In vitro drug release studies were carried out by using the Franz diffusion cell. The cumulative % of drug released in 10 hours from the six batch formulations were 95.66%, 94.2%, 97.33%, 90.13%, 83.75% and 85.71%, respectively. On the basis of in-vitro drug release, formulation (HE-2) was found to be better than other formulation and these were selected for further evaluation such as anti-fungal activity and stability studies.
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De Marco, Iolanda. "Transdermal Patches Containing Opioids in the Treatment of Patients with Chronic Pain." Processes 11, no. 9 (2023): 2673. http://dx.doi.org/10.3390/pr11092673.
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Transdermal delivery is a non-invasive route, used as an alternative to the oral route, to administer drugs through the skin surface. One of the fields in which they are particularly used is that of pain therapy. In this treatment, transdermal patches, particularly those containing opioids, are used to complement or replace orally administered drugs. First-generation patches are constituted by reservoir systems, where the drug is dissolved in a solvent and gelled with a polymer. In contrast, the active principle is incorporated into the polymer adhesive in more recent matrix patches. In this review, the main papers related to the production and employment of transdermal patches containing the two most used opioids, i.e., fentanyl and buprenorphine, have been critically analyzed. From the analysis of the literature, it is possible to deduce that the type of drug and the amount of drug present in the patch must be chosen not according to the origin of the pain but to the age of the patient, the area where the patch is applied, and the frequency at which the patch is replaced.
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Raktimava Das Sarkar and Gouranga Sundar Roy. "Optimised herbal transdermal patch of ethnobotanical plant Costus igneus N. E. br. Developed through response surface methodology." Open Access Research Journal of Biology and Pharmacy 9, no. 3 (2023): 041–56. http://dx.doi.org/10.53022/oarjbp.2023.9.2.0055.
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Costus igneus (Family: Costaceae) has been used by the aboriginal humans since long through oral route. In our laboratory, we used biodegradable polymer for release control of this transdermal patch. This transdermal patch could be affixed in the lower abdominal region which releases intraperitoneally after principal meals, twice a day; which could be terminated instantly by removing the patch externally. Our objective is Formulation, evaluation and statistical designing of a Transdermal patch containing ethnobotanical plant Costus igneus. As Transdermal Patch reduces can be removed when termination of treatment is necessary and it also has the capability to bypass the different chemical changes that a oral pill has to go through. The Macro-physico evaluation parameters were calculated. The folding endurance was in between of 7 to 16, the maximum value was of the FOPT, the Tensile strength was relatively similar in all the formulations. FOPT showed the highest of all. In percentage elongation test the FOPT showed good resilience, thickness was relatively acceptable for all the formulations. % moisture content and %moisture uptake was acceptable in all of the formulations showed a good and satisfiable range. The drug content was calculated according the total quercetin content taking pure quercetin API as the reference FOPT had the highest drug content of 82.5%. The Response Surface Curve predicted the optimised formulation and the desirability score also gives us our optimised patch. The Kinetics for the optimum by the optimization of transdermal patch was observed in all the different type of plots. The FOPT had a good linearity of 0.938 in regression co-efficient with Korsmeyer-Peppas Plot . It explains the release of drug’s material through a polymeric matrix system while also considering Non-Fickian drug release mechanism. The different Response Surface Curve allows us to predict from the software that the FOPT Formulation is the Gem of Ten. This would produce beneficial blood-sugar content reduction. If we can commercialise this Herbal Transdermal Patch then, it can be an innovation remedy for this chronic disease.
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Ganti, Sindhu S., Sonalika A. Bhattaccharjee, Kevin S. Murnane, Bruce E. Blough, and Ajay K. Banga. "Formulation and evaluation of 4-benzylpiperidine drug-in-adhesive matrix type transdermal patch." International Journal of Pharmaceutics 550, no. 1-2 (2018): 71–78. http://dx.doi.org/10.1016/j.ijpharm.2018.08.033.
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Dileep, Kumar Awasthi, B. Puranik Sangamesh, Saraswat Rohit, and Arya Priya. "Design and Evaluation of Transdermal Patches of Labetalol Hydrochloride." International Multispeciality Journal of Health 6, no. 8 (2020): 15–30. https://doi.org/10.5281/zenodo.4117428.
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<strong>Abstract</strong><strong>—</strong> β-blockers like labetalol hydrochloride (LHCl) are potent and highly effective antihypertensive agents. The main drawback associated with β-blockers is extensive first-pass metabolism, variable bioavailability requiring frequent dose administration. This makes them an ideal candidate for transdermal therapeutic systems. β-blockers formulated as transdermal therapeutic system should enhance the bioavailability as well as improve patient compliance. Constant innovations and improvement in this field have potential that large-scale commercialization of transdermal dosage forms can be done. <strong>Aim: </strong>The aim of the present work was to develop and evaluate matrix type transdermal patches containing new polymeric combination to enhance the bioavailability as well as improve patient compliance. <strong>Materials and Methods: </strong>In present work development and evaluation of matrix-type transdermal patches containing a new polymeric combination of HPMC, carbopol934, ethyl cellulose, propylene glycol, polyethylene glycol, and isopropyl myristate for labetalol (LHCl) HCl (LBHCl). Film casting technique has been used in preparing patches. The patches were characterized for physical, in vitro release studies and ex vivo permeation studies using human cadaver skin. <strong>Result: </strong>F<sub>6 </sub>was found to be better than the other formulations and hence selected as the optimized formulation on the basis of results of evaluating parameters such as thickness, flatness, folding endurance, tensile strength, moisture content, moisture uptake, and drug content, formulation. The optimized patch was assessed for its pharmacokinetic, pharmacodynamic, skin irritation test and stability studies. <strong>Conclusion: </strong>Successful development of sustained release matrix type of transdermal patches which can show greater patient compliance in treating hypertension has been done.
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Bariki Rajasekhar, B Harish Reddy, G Aiman Farheen, et al. "Formulation and evaluation of transdermal patch of carbamazepine." World Journal of Advanced Research and Reviews 22, no. 2 (2024): 1601–11. http://dx.doi.org/10.30574/wjarr.2024.22.2.1549.
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Transdermal drug delivery system (TDDS) is a widely accepted mode of drug delivery method due to various advantages and one of the novel routes for systemic delivery of drugs through intact skin. Topical drug administration is a systemic and localized method of delivering drugs through skin and is considered an attractive alternative to oral and parenteral routes. The aim of present study was to formulate and evaluate Matrix type transdermal drug delivery system (TDDS) of Carbamazepine was prepared by the solvent evaporation technique. Several batches were prepared by using combination of HPMC E-15, Eudragit RL-100, and Ethyl Cellulose different ratios. Propylene glycol was used as plasticizer and DMSO was incorporated as a permeation enhancer. These Formulated transdermal patches were characterized for their physicochemical parameters like thickness, weight variation, folding endurance, percentage moisture uptake, Percentage moisture uptake and In vitro drug release studies were examined. Among the above all formulation F6 was chosen as a best Formulation, because this optimised formulation showed satisfactory drug content, physical characteristic for its thickness, weight uniformity, percentage moisture content, percentage moisture uptake, and maximum % of drug release i.e., 93.95 % in 12 hours. The optimized formulation (F6) showed maximum highest percentage of drug release.
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Bariki, Rajasekhar, Harish Reddy B, Aiman Farheen G, et al. "Formulation and evaluation of transdermal patch of carbamazepine." World Journal of Advanced Research and Reviews 22, no. 2 (2024): 1601–11. https://doi.org/10.5281/zenodo.14701877.
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Transdermal drug delivery system (TDDS) is a widely accepted mode of drug delivery method due to various advantages and one of the novel routes for systemic delivery of drugs through intact skin. Topical drug administration is a systemic and localized method of delivering drugs through skin and is considered an attractive alternative to oral and parenteral routes. The aim of present study was to formulate and evaluate Matrix type transdermal drug delivery system (TDDS) of Carbamazepine was prepared by the solvent evaporation technique. Several batches were prepared by using combination of HPMC E-15, Eudragit RL-100, and Ethyl Cellulose different ratios. Propylene glycol was used as plasticizer and DMSO was incorporated as a permeation enhancer. These Formulated transdermal patches were characterized for their physicochemical parameters like thickness, weight variation, folding endurance, percentage moisture uptake, Percentage moisture uptake and In vitro drug release studies were examined. Among the above all formulation F6 was chosen as a best Formulation, because this optimised formulation showed satisfactory drug content, physical characteristic for its thickness, weight uniformity, percentage moisture content, percentage moisture uptake, and maximum % of drug release i.e., 93.95 % in 12 hours. The optimized formulation (F6) showed maximum highest percentage of drug release.
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Rathore, Vijendra Pal Singh, Komal Tikariya, and Jayanti Mukherjee. "Formulation and Evaluation of Transdermal Patch of Thiochochicoside." International Journal of Pharmaceutical Sciences and Medicine 6, no. 12 (2021): 18–28. http://dx.doi.org/10.47760/ijpsm.2021.v06i12.002.
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The aim of the study is to formulate and evaluate transdermal patches of Thiocholchicoside In the present study, matrix type were prepared by moulding techniques. This mode of drug delivery is more beneficial for chronic disorders such as Rheumatoid arthritis which require long term drug administration to maintain therapeutic drug concentration in plasma. Transport of drugs or compounds via skin is a complex phenomenon, which allows the passage of drugs or compounds into and across the skin. In the present work an attempt has been made to formulate and evaluate the transdermal patches of Thiocholchicoside using various blends of polymer. The polymeric combinations EC/PVP and EC/HPMC used for the formulation of transdermal patches showed good film forming property. The patches formed were thin, flexible, smooth and transparent. The weight variation tests showed less variation in weight and suggesting uniform distribution of drug and polymer over the mercury surface. The thicknesses of the transdermal patches were found to increase on increasing concentration of hydrophilic polymers like PVP and HPMC.All the patches showed good flexibility and folding endurance properties. The result suggests that the formulations with increased hydrophilic polymer concentration showed long folding endurance. The moisture content in the patches was found to be low and formulations with more hydrophilic polymer concentrations showed more percentage moisture content. The in-vitro drug release studies showed that formulations TDP2, TDP3, TDP4, and TDP5 with increased concentration of hydrophilic polymer showed rapid release. The drug content analysis showed minimum variations suggesting uniform distribution of drug.
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Jalhan, Sunny, Khushpal Kaur, Preetinder Kaur, and Upendra K Jain. "FORMULATION AND IN-VITRO EVALUATION OF TRANSDERMAL MATRIX PATCHES OF DOXOPHYLLINE." Asian Journal of Pharmaceutical and Clinical Research 9, no. 5 (2016): 140. http://dx.doi.org/10.22159/ajpcr.2016.v9i5.12774.
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ABSTRACT Objective: The objective of the present study was to fabricate matrix type transdermal patch with varied proportion of hydrophilic (HPMC E-50) and (PVP) combination incorporating the drug Doxophylline and to execute the physicochemical and in vitro assessment. The motive was to provide the delivery of Doxophylline at a controlled rate across the intact skin to attain a therapeutically effective drug level for a longer time span from transdermal matrix patch.Method: Prefomulation studies and evaluation was done by using different parameter such as Partition coefficient, Physicochemical Compatibility of Drug and Polymer, Physical appearance, Thickness Measurement, Folding Endurance, Weight variation, Percentage moisture lost, Percentage moisture uptake, Drug content Determination.Result: The results shows that patches of Doxophylline obtained by the solvent evaporation method had acceptable physicochemical characteristics and satisfactory percentage drug release. Conclusion: The main conclusion of my work was formulating the Doxophylline transdermal system was to prolong the drug release time, reduce the frequency of administration and to improve patient compliance. Six formulations were prepared using two polymers in different ratios along with plasticizers and penetration enhancer.
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Kumar, Sanjay, Anirudh Singh Deora, Narahari KV, and Tanveer Shaikh. "Optimizing Transdermal Patch Design: A Quality by Design Approach for Dysmenorrhea Relief." INTERNATIONAL JOURNAL OF DRUG DELIVERY TECHNOLOGY 14, no. 03 (2024): 1299–305. http://dx.doi.org/10.25258/ijddt.14.3.07.
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This study explores the potential of transdermal patches as a systemic delivery system for donepezil (DPZ), aiming to circumvent hepatic first-pass metabolism and mitigate oral administration-associated side effects. DPZ, known for its poor solubility and adverse effects, is formulated into transdermal patches using a matrix-type approach with PVP K30 and HPMC K100 polymers alongside dimethyl sulfoxide as a plasticizer. Through solvent casting on a mercury surface, the patches are prepared and assessed for physical properties and drug-excipient interactions using FTIR analysis. The results demonstrate satisfactory physical characteristics, including appearance, weight variation, and tensile strength. Notably, formulations containing HPMC K100 (400 mg) and PVP K30 (300 mg) exhibit enhanced DPZ discharge, signifying their potential as an effective drug delivery system for mitigating DPZ-associated side effects.
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Shayeda, Dr, and Nusrat Ayesha. "Development of Tizanidine HCl transdermal patches: In-vitro and Ex-vivo characterization." Journal of Drug Delivery and Therapeutics 9, no. 1-s (2019): 295–300. http://dx.doi.org/10.22270/jddt.v9i1-s.2431.
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The purpose of this work was to design and evaluate matrix type transdermal patches of Tizanidine hydrochloride using Hypromellose (HPMC E15) as polymer, dibutyl phthalate as plasticizer and citral as permeation enhancer. The DSC and FTIR results showed the compatibility of the excipients with the drug. These transdermal drug delivery systems were characterized for their thickness, folding endurance, content uniformity, tensile strength and in-vitro release studies of the drug from the polymeric matrix. In-vitro release studies and ex-vivo permeation were carried out with modified Franz diffusion cell using pH 5.8 & pH 7.4 phosphate buffers as receptor medium and it showed controlled release of drug. The results suggest that the formulation of TIZ may be useful in the development of a therapeutic system to deliver TIZ across the skin for a prolonged period, i.e. 24 hr.
 Keywords: Tizanidine Hydrochloride, Transdermal patch, HPMC E15, in-vitro & ex-vivo.
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Kharia, A., R. Gilhotra, and A. K. Singhai. "Overview of Transdermal Medicated Patches with its research updates in preceding years." Journal of Drug Delivery and Therapeutics 9, no. 3-s (2019): 1094–102. http://dx.doi.org/10.22270/jddt.v9i3-s.2962.
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Innovations in transdermal drug delivery systems (TDDS) is an important influence to medical practice by providing advances in the delivery of treatment with existing conventional drugs and novel drugs. Transdermal drug delivery is one of the most promising methods for drug application. It has several benefits over conventional system to offer sustained drug release, avoidance of first pass effect, patient compliance, ease of application and removal in case of toxicity as well as decrease in the side effects as compared with conventional therapy. Transdermal patches are dosage forms which transport drug to viable epidermal and dermal tissues of the skin for local therapeutic effect while a very major fraction of drug is transported into the systemic blood circulation. Skin penetration enhancement techniques have been developed to improve bioavailability and increase the range of drugs for which topical and transdermal delivery. The purpose of this review is to introduce transdermal patches including type of transdermal patches, components of transdermal patches, method of preparation of TDDS, evaluation parameters, researches and development done on TDDS in last decade etc. Keywords: Transdermal Drug Delivery System, Permeation Enhancers, Transdermal Patch, Polymer Matrix.
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Devi, Kusum, and K. L. K. Paranjothy. "Pharmacokinetic Profile of a New Matrix-Type Transdermal Delivery System: Diclofenac Diethyl Ammonium Patch." Drug Development and Industrial Pharmacy 25, no. 5 (1999): 695–700. http://dx.doi.org/10.1081/ddc-100102228.
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Järvinen, Asko, Ann-Christine Bäckström, Charlotta Elfström, and Antti Viitanen. "Comparative absorption and variability in absorption of estradiol from a transdermal gel and a novel matrix-type transdermal patch." Maturitas 38, no. 2 (2001): 189–96. http://dx.doi.org/10.1016/s0378-5122(00)00222-x.
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Reddyy, P. Srikanth, V. Alagarsamy, P. Subhash Chandra Bose, V. Sruthi, and D. Saritha. "Formulation and Evaluation of Naproxen Sodium Transdermal Patches Using Natural Polymer." International Journal of Medical and Biomedical Studies 8, no. 1 (2024): 11–21. http://dx.doi.org/10.32553/ijmbs.v8i1.2765.
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Natural polymer from flaxseed Linum usitatissimum was used in this study to develop a matrix-dispersion type transdermal Naproxen sodium medication delivery system. Flaxseed mucilage and hydroxyl propyl methyl cellulose were used to make transdermal patches of naproxen sodium. Transdermal patches were made using flaxseed mucilage, whichwas adopted and tested for its impact on patch quality. The solubility, melting point, and partition coefficient of the medication have been determined as preliminary evaluation metrics. Using Franz diffusion cells, the produced patcheswere assessed in vitro for in vitro drug release, folding durability, thickness, and weight fluctuation of the patches. For FTIR and DSC, and a stability analysis, the improved formulation was used. Data from FTIR and DSC demonstrated that the medication and excipient had no significant interaction. Keywords: naproxen sodium, flaxseed mucilage, solvent casting method, folding endurance, Franz diffusion cell.
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Kamble, M. D., B. V. Dhokchawle, and S. J. Tauro. "FORMULATION AND EVALUATION OF TRANSDERMAL DRUG DELIVERY SYSTEM OF ATENOLOL USING CHITOSAN." INDIAN DRUGS 51, no. 04 (2014): 36–41. http://dx.doi.org/10.53879/id.51.04.10095.
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The effect of various concentrations of chitosan as a polymer was investigated for the transdermal delivery of atenolol across human cadaver skin by using dimethylsulfoxide as a penetration enhancer. Atenolol-chitosan matrix type patches were formulated using different polymer concentrations. Atenolol at a fixed concentration of 10 mg was added in polymer and dibutyl phthalate, 30% w/w of polymer, was added as a plasticizer. All the transdermal patches were evaluated for thickness, weight variation, folding endurance, breaking force, and percent moisture content. The comparative study of release kinetics with different polymer ratios showed that the patch containing drug polymer ratio 1:7 had maximum release of drug (81.92%) and all its physicochemical parameters were within the acceptable limit.
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Kamble, M. D., B. V. Dhokchawle, and S. J. Tauro. "FORMULATION AND EVALUATION OF TRANSDERMAL DRUG DELIVERY SYSTEM OF ATENOLOL USING CHITOSAN." INDIAN DRUGS 51, no. 04 (2014): 36–41. http://dx.doi.org/10.53879/id.51.04.10095.
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The effect of various concentrations of chitosan as a polymer was investigated for the transdermal delivery of atenolol across human cadaver skin by using dimethylsulfoxide as a penetration enhancer. Atenolol-chitosan matrix type patches were formulated using different polymer concentrations. Atenolol at a fixed concentration of 10 mg was added in polymer and dibutyl phthalate, 30% w/w of polymer, was added as a plasticizer. All the transdermal patches were evaluated for thickness, weight variation, folding endurance, breaking force, and percent moisture content. The comparative study of release kinetics with different polymer ratios showed that the patch containing drug polymer ratio 1:7 had maximum release of drug (81.92%) and all its physicochemical parameters were within the acceptable limit.
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Chauhan, Shikha Baghel, Tanveer Naved, and Nayyar Parvez. "FORMULATION AND DEVELOPMENT OF TRANSDERMAL DRUG DELIVERY SYSTEM OF ETHINYLESTRADIOL AND TESTOSTERONE: IN VITRO EVALUATION." International Journal of Applied Pharmaceutics 11, no. 1 (2019): 55. http://dx.doi.org/10.22159/ijap.2019v11i1.28564.
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Objective: The combination therapy of ethinylestradiol and testosterone in post-menopausal females has shown improved sexual response and libido. The present studies were designed to develop a suitable matrix-type transdermal drug delivery system (TDDS) of ethinylestradiol and testosterone using the polymer chitosan.Methods: Five formulations (ET1 to ET5) were developed by varying the concentration of polymer and keeping the drug load constant. Physical parameters and drug excipient interaction studies were evaluated in all the formulations. In vitro skin permeation profiles of ethinylestradiol and testosterone from various formulations were simultaneously characterized in a thermostatically controlled modified Franz Diffusion cell using HPLC. Based on the physical parameters and in vitro skin permeation profile formulation ET3 containing 30 mg/ml of chitosan was found to be the best and chosen for further studies. Optimized formulation was subjected to in vivo pharmacokinetic analysis in rats using ELISA.Results: Stability profile of patch formulation ET3 depicted stability up to 3 mo. One week skin irritation evaluation in rats indicated that formulation ET3 was nonirritating. Combination transdermal patch across rat skin showed a maximum release of 92.936 and 95.03 % in 60 h with a flux of 2.088 and 21.398 µg/cm2h for ethinylestradiol and testosterone respectively.Conclusion: The net result of this study is the formulation of a stable, non-irritating transdermal patch of ethinylestradiol and testosterone, with good bioavailability and can be used as Estrogen Replacement Therapy (ERT) in postmenopausal women.
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Wang, Zejun, Jinqiang Wang, Hongjun Li, et al. "Dual self-regulated delivery of insulin and glucagon by a hybrid patch." Proceedings of the National Academy of Sciences 117, no. 47 (2020): 29512–17. http://dx.doi.org/10.1073/pnas.2011099117.
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Reduced β-cell function and insulin deficiency are hallmarks of diabetes mellitus, which is often accompanied by the malfunction of glucagon-secreting α-cells. While insulin therapy has been developed to treat insulin deficiency, the on-demand supplementation of glucagon for acute hypoglycemia treatment remains inadequate. Here, we describe a transdermal patch that mimics the inherent counterregulatory effects of β-cells and α-cells for blood glucose management by dynamically releasing insulin or glucagon. The two modules share a copolymerized matrix but comprise different ratios of the key monomers to be “dually responsive” to both hyper- and hypoglycemic conditions. In a type 1 diabetic mouse model, the hybrid patch effectively controls hyperglycemia while minimizing the occurrence of hypoglycemia in the setting of insulin therapy with simulated delayed meal or insulin overdose.
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Hardainiyan, Swati, Krishan Kumar, Bankim Chandra Nandy, and Richa Saxena. "DESIGN, FORMULATION AND IN VITRO DRUG RELEASE FROM TRANSDERMAL PATCHES CONTAINING IMIPRAMINE HYDROCHLORIDE AS MODEL DRUG." International Journal of Pharmacy and Pharmaceutical Sciences 9, no. 6 (2017): 220. http://dx.doi.org/10.22159/ijpps.2017v9i6.16851.
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Objective: The aim of the present investigation was to form matrix type transdermal patches containing imipramine hydrochloride were prepared using two polymers by solvent evaporation technique to minimise the dose of the drug for lesser side effect and increase the bioavailability of a drug.Methods: In the present study, drug loaded matrix type transdermal films of imipramine hydrochloride were prepared by the solvent evaporation method with the help of polymers along with polyethene glycol (PEG) 400 was used as plasticizer and dimethyl sulfoxide (DMSO) was used as penetration enhancer. Drug-polymer interactions determine by FTIR and a standard calibration curve of imipramine hydrochloride was determined by using UV estimation.Results: The formulated transdermal patch by using PVP K-30, HPMC K100M showed good physical properties. All prepared formulations indicated good physical stability. The formulation F-1 gave the most suitable transdermal film with all desirable physicochemical properties. The thickness of the patches was varied from 0.263±0.67 mm to 0.301±0.61 mm, uniformity of patches showed that patches prepared by solvent evaporation while low standard deviation values ensued by thickness measurements of the film, and weights ranged between 50.5±0.75 mg and 52.15±2.15 mg, which indicates that different batches patch weights, were comparatively similar. Folding endurance was found to be>200 that is satisfactory for the patches, drug content was found to be 5.33±0.14 mg to 5.57±0.095 mg. In vitro, drug permeation studies of formulations were performed by using K-C diffusion cells using abdomen skin of the albino rat. The results were best in in-vitro skin permeation through rat skin as compared to all other formulations prepared with a hydrophilic polymer containing permeation enhancer. The formulation, F1 is considered as the best formulation, since it shows maximum in vitro drug release as 84.71±3.07 % at 24 h. The drug release kinetics studies showed that the majority of formulations were governed by Higuchi model and mechanism of release was non-Fickian mediated.Conclusion: In conclusion, controlled release transdermal drug delivery system (TDDS) patches of imipramine hydrochloride can be prepared using the polymer combinations, with plasticizer and enhancer. The release rate of drug through patched increased simultaneously as the concentration of hydrophilic polymer was increased. However, the mechanism of drug release of all formulations was non-Fickian. The properties of a film did not change during the period of study.
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Ossowicz-Rupniewska, Paula, Paulina Bednarczyk, Małgorzata Nowak, et al. "Evaluation of the Structural Modification of Ibuprofen on the Penetration Release of Ibuprofen from a Drug-in-Adhesive Matrix Type Transdermal Patch." International Journal of Molecular Sciences 23, no. 14 (2022): 7752. http://dx.doi.org/10.3390/ijms23147752.
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This study aimed to evaluate the effect of chemical modifications of the structure of active compounds on the skin permeation and accumulation of ibuprofen [IBU] from the acrylic pressure-sensitive adhesive used as a drug-in-adhesives matrix type transdermal patch. The active substances tested were ibuprofen salts obtained by pairing the ibuprofen anion with organic cations, such as amino acid isopropyl esters. The structural modification of ibuprofen tested were Ibuprofen sodium salt, [GlyOiPr][IBU], [AlaOiPr][IBU], [ValOiPr][IBU], [SerOiPr][IBU], [ThrOiPr][IBU], [(AspOiPr)2][IBU], [LysOiPr][IBU], [LysOiPr][IBU]2, [PheOiPr][IBU], and [ProOiPr][IBU]. For comparison, the penetration of unmodified ibuprofen and commercially available patches was also investigated. Thus, twelve transdermal patches with new drug modifications have been developed whose adhesive carrier is an acrylate copolymer. The obtained patches were characterized for their adhesive properties and tested for permeability of the active substance. Our results show that the obtained ibuprofen patches demonstrate similar permeability to commercial patches compared to those with structural modifications of ibuprofen. However, these modified patches show an increased drug permeability of 2.3 to even 6.4 times greater than unmodified ibuprofen. Increasing the permeability of the active substance and properties such as adhesion, cohesion, and tack make the obtained patches an excellent alternative to commercial patches containing ibuprofen.
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Hendradi, Esti, Rahayuningtyas, and Tristiana Erawati. "The Effect of Polymers Ratio Carboxymethyl Chitosan, Polyvinyl Pyrolidone K-30, and Ethyl Cellulose N22 on Physico-Chemical Characteristics and Drug Release from Matrix Type Diclofenac Potassium Patch." JURNAL FARMASI DAN ILMU KEFARMASIAN INDONESIA 10, no. 1 (2023): 54–61. http://dx.doi.org/10.20473/jfiki.v10i12023.54-61.
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Background: Diclofenac potassium is an NSAID drug that is used in the treatment of mild to moderate pain. The use of this drug orally can cause side effects in the gastrointestinal tract, and the drug will undergo extensive first-pass metabolism in the liver. Therefore, preparations for transdermal patches were made. Objective: Determining the effect of the polymer ratios of carboxymethyl chitosan, polyvinyl pyrolidone K-30, and ethyl cellulose N22 on the physicochemical characteristics and drug release of a matrix type diclofenac potassium patch. Methods: In this study, matrix type diclofenac potassium patches were made using a combination of carboxymethyl chitosan (CMC), polyvinyl pyrrolidone (PVP) K-30 polymer, and ethyl cellulose (EC) N22 in a ratio of 2:3:7 and 3:2:7. Patches are made by mixing the entire polymer matrix and diclofenac potassium together, which are then evaporated and dried. Results: The results showed that the different polymer compositions of CMC, PVP K-30, and EC N22 resulted in patches with physicochemical characteristics that were not significantly different. The combination of these polymers is able to control the release of the drug from the patch for a long time. It was also found that increasing the concentration of CMC was able to increase the rate of release of diclofenac potassium. Formula 2 with a ratio of 3:2:7 is claimed to be the best formula in terms of physical, chemical, and drug release characteristics from the patch. Further studies are needed, such as drug penetration tests into the skin.
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Sellers, MD, PhD, FRCPC, Edward M., Reinhard Schuller, MSc, Myroslava K. Romach, MD, and G. L. A. Horbay, PhD. "Relative abuse potential of opioid formulations in Canada: A structured field study." Journal of Opioid Management 2, no. 4 (2006): 219. http://dx.doi.org/10.5055/jom.2006.0034.
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Introduction: While prescription opioids can improve quality of life through pain relief, they are susceptible to misuse. This field study characterizes the relative susceptibility and attractiveness of a new analgesic patch, with fentanyl embedded in a matrix material, compared to other opioid dose formulations.Methods: Recreational opioid abusers (N = 42; 31 male, 11 female) from three Canadian sites participated in structured interviews. They were presented with nine products, some of which were hypothetical (fentanyl [F], hydromorphone [H], and oxycodone [O] in each of three formulations: matrix patch [M], reservoir-type gel patch [G], and tablet [T]). The attractiveness and tampering potential of each product was ranked using two 7-point Likert scales (Value of Product and Likelihood to Tamper), an index representing the product of the two scales, a 17-item Opiate Attractiveness Scale (OAS), relative street value, and rank order of overall desirability. Non-parametric analyses were used to compare each product to the FM.Results: The FT, HT, and FM were highly valued and most likely to be tampered with. The products were ranked in decreasing order of desirability as follows: FT > HT > FM > FG > OT > HM > HG > OM > OG. On the OAS, FM was more attractive than all gel-patch products (p < 0.001), and OT was most attractive overall. FM was statistically similar to OT, FT, OM, and HT. Of the 42 subjects, 25 (60 percent) preferred the matrix patch to the gel patch. Of the 17 subjects who preferred the gel patch, 10 (59 percent) were from a region generally unfamiliar with that formulation.Conclusions: Fentanyl is attractive to opioid abusers regardless of formulation. In Canada, a fentanyl matrix patch may be at higher risk for diversion, tampering, and abuse than other transdermal opioid formulations. These findings should be confirmed by epidemiological studies. Comparative risk management programs should be part of the development of any new narcotic delivery system.
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Hamdan, Lama, and Jamila Husian. "FORMULATION AND EVALUATION IN VITRO A MATRIX TYPE OF KETOTIFEN FUMARATE TRANSDERMAL PATCHES FOR ALLERGIC DISEASES." Asian Journal of Pharmaceutical and Clinical Research 10, no. 10 (2017): 327. http://dx.doi.org/10.22159/ajpcr.2017.v10i10.20123.
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Objective: Transdermal patches of Ketotifen fumarate (KT) were developed for prolonged effect of the drug, and to protect the patient from allergic symptoms associated with asthma and other allergic diseases.Methods: Matrix type patches were prepared by solvent casting technique using different types of polymers: Hydroxy propyl methyl cellulose (HPMC K15M) and ethyl cellulose to formed the matrix of the patch in different ratios, emulsifying agents were added as a penetration enhancers (Span 60, Tween 60, Cremophor EL) in a ratio 0.025% w/v to the matrix, 10% v/v of glycerin was added as plasticizer to 10 ml of chloroform:methanol (1:1). The drug matrix film was casted on a polyvinyl alcohol backing membrane. All patches were evaluated for physical proprieties, thickness uniformity, folding endurance, moisture uptake, moisture content, drug content, uniformity of weight, content uniformity, in vitro drug release, and kinetic models. Differential scanning calorimetry was used to characterize physical mixtures of KT and the different used excipients.Results: The results showed that the prepared patches had acceptable physical properties. The drug substance was released well. Adding the penetration enhancers delayed the release of the drug from the matrix in all the prepared formulas, formula A2 that having no enhancer, showed maximum amounts of drugs release (90.06±0.9)% for 24 hrs. However, adding penetration enhancers decreased the amount of the drug release, formula B2 having Tween 60 as a penetration enhancer, showed the maximum release of the drug (87.78±0.88)%, and formula B3 having Cremophor EL showed the minimum release of the drug (79.13±1.58) at the end of 24 hrs dissolution study. The release of the drug from all formulations was followed by Korsmeyer-Peppas pattern with n>0.45 indicating that drug release from matrix was mainly happened by swallowed and diffusion (non- Fickian pattern).Conclusion: Optimized formula A2 containing the maximum amounts of HPMC K15M showed a controlled release of the drug over 12 hrs, and it identified as a successful formulation for this study.
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Kuznetsova, E. G., L. A. Salomatina, O. M. Kuryleva, Yu B. Basok, and V. I. Sevastianov. "Transcutaneous permeation enhancer complex for polymer-based transdermal patches." Russian Journal of Transplantology and Artificial Organs 27, no. 1 (2024): 188–97. https://doi.org/10.15825/1995-1191-2025-1-188-197.
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Selecting a permeation enhancer complex (PEC) for inclusion in a matrix-type transdermal patch (TP) is a primary task in creating a new dosage form with percutaneous administration. Objective: to develop a biologically safe PEC capable of regulating percutaneous diffusion of low-molecular-weight drugs from the polyacrylate matrix of a TP and without causing adverse skin reactions. Materials and methods. The PEC contained apricot kernel oil, dioctyl sodium sulfosuccinate, dihydroquercetin and alpha-tocopherol acetate – substances that have a good impact on the functional properties of polymer-based TPs. Low-molecular alcohol-soluble drugs (chlorpropamide, caffeine and sodium benzoate and lidocaine hydrochloride) used to treat diseases of various etiologies were used as active ingredients. In vitro studies of percutaneous drug delivery were carried out on male Chinchilla rabbits in Franz glass diffusion cells using a drug diffusion analyzer. Using spectrophotometry and high-performance liquid chromatography, concentrations of drugs in aqueous solutions and in the blood plasma of the laboratory animals were measured. The irritant effect of the lidocaine-loaded transdermal polymeric matrix was tested on sexually mature young male New Zealand White rabbits. Results. When PEC was introduced into the polymer matrix film, percutaneous diffusion of the drugs increased significantly from 2.1 ± 0.4 to 9.2 ± 1.4 mg over 24 hours of experiment for the chlorpropamide-loaded TP and from 9.2 ± 1.2 to 35.2 ± 7.5 mg for the caffeine-loaded TP. Additionally, there was a 1.7- and 2.9-fold decrease and a 2.3- and 2.7-fold increase in the time to reach a constant drug concentration in blood for the chlorpropamide- and caffeine-containing TPs, respectively. Using the lidocaine- and chlorpropamide-loaded TPs, it was shown that the presence of PEC in the polymer matrix film causes no skin irritation and that the shelf life of the transdermal form increases from 1 to 3 years. Conclusion. Introduction of the proposed PEC into the polymeric matrixes of TPs enhanced percutaneous diffusion of the drugs, reduced skin irritation from the TP components, and increased the shelf life of the finished dosage forms.
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Otterbach, Anna, and Alf Lamprecht. "Enhanced Skin Permeation of Estradiol by Dimethyl Sulfoxide Containing Transdermal Patches." Pharmaceutics 13, no. 3 (2021): 320. http://dx.doi.org/10.3390/pharmaceutics13030320.
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Dimethyl sulfoxide is a well-known and widely used dermal penetration enhancer. Its incorporation in transdermal patches would be highly desirable; however, due to its volatility this is extremely challenging. Here, we report on the feasibility of a dimethyl sulfoxide (DMSO) containing transdermal system containing estradiol as a model compound. Transdermal patches were prepared from duro-tak® 387-2510 containing various DMSO concentrations at different drying temperatures. The resulting patches were analyzed for DMSO content, estradiol and DMSO release, estradiol and DMSO permeation through excised porcine skin, and recrystallization during stability testing. Drying conditions in the range of 35° to 40° allowed a complete polymer solvents removal while retaining significant amounts of DMSO (≤10 mg/patch). Estradiol skin permeation increased 4-fold (Jss = 4.12 µg/cm−2·h−1) compared to DMSO-negative control (Jss = 1.1 ± 0.2 µg/cm−2·h−1). As additional benefit, estradiol recrystallization was inhibited by DMSO at even lowest solvent concentrations. Storage stability was limited to 6 months at 25 °C with a surprising discrepancy between DMSO content (significantly lower) and flux (not significantly different). Although the technical feasibility range is relatively narrow, such DMSO-containing matrix-type patches are able to significantly enhance drug permeation through the skin while ameliorating the product stability against recrystallization.
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Ermawati, Dian Eka, Anif Nur Artanti, Dyah Ayu Ambarwati, Niken Rosyana Dewi Septini, Sholichah Rohmani, and Wisnu Kundarto. "STUDY OF KINETICS MODEL OF FLAVONOID TOTAL RELEASE IN PATCH OF ANTIHYPERTENSIVE HERBS." Journal of Pharmaceutical Sciences and Community 18, no. 1 (2021): 7–14. http://dx.doi.org/10.24071/jpsc.002203.
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The liquid extract of antihypertensive herbs could reduce blood pressure equivalent to Hydrochlorothiazide 25 mg based on research conducted in “Hortus Medicus” clinic, Tawangmangu, Central Java, but parameters of herbal medicine taste, design, and packaging had the lowest scores. Transdermal patch was chosen as an alternative to resolve those problems. Polymers determined the effectiveness of the active substance release from the formula. Patch was formulated from combination of hydrophilic hydroxy methylcellulose (HPMC) and carboxymethylcellulose natrium (CMC-Na) polymer which would produce a fast release profile. The objective of this research was to study the kinetics models of total flavonoid release and to study the total number of flavonoids released from the antihypertensive herbs patch for 5 hours, as well as to determine the optimum formula for observing the weight, pH and loss on drying. Herbs were infused with distilled water at 90 ° C for 15 minutes, filtered then evaporated. Release kinetics model used a modified type-5 dissolution apparatus equipment with a cellophane membrane. The optimum proportion of HPMC and CMC-Na was 220:180 mg. Patch was dark brown, circle shaped, moist and flexible. It had pH value of 7.29 ± 0.09, folding endurance of >350, and thickness of 0.64 ± 0.05 mm. The average percentage of total flavonoids released from the matrix patch was 37.23% for 5 hours. The release kinetics followed the Higuchi kinetics model with a diffusion mechanism.
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Sheppard, Brian, Lucy Norris, and Jeanette Brosnan. "Haemostatic activation in post-menopausal women taking low-dose hormone therapy: Less effect with transdermal administration?" Thrombosis and Haemostasis 97, no. 04 (2007): 558–65. http://dx.doi.org/10.1160/th06-10-0567.
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SummaryHormone therapy (HT) increases the risk of cardiovascular and thromboembolic disease in post-menopausal women. Recent studies have suggested that prothrombotic mechanisms are likely to be involved. Transdermal HT avoids the first-pass effect of oestrogen in the liver and may have a less marked effect on the haemostatic system than equivalent oral preparations. The majority of studies have compared HT preparations that have different formulations as well as routes of administration. We investigated changes in the haemostatic system in post-menopausal women using two pharmacologically similar HT preparations, which differed only in their route of administration. Three hundred forty-four healthy post-menopausal women were randomised to six months treatment with either a transdermal matrix patch containing 25 µg 17 β -estradiol/125 µg norethisterone acetate (NETA) applied every 3–4 days, or an equivalent oral preparation (estradiol 1mg and NETA 0.5 mg given once daily). Oral treatment significantly reduced fibrinogen (p<0.003), factor VIIc (FVIIc) (p<0.00001), and antithrombin (AT) levels (p<0.005); the effects in the transdermal group were less marked with no reduction in fibrinogen levels and lesser effect on FVIIc (p<0.03) compared with oral treatment. Treatment type significantly affected fibrinolysis with lower plasminanti- plasmin (PAP) levels in the transdermal group (p<0.003) and lower plasminogen activator inhibitor-1 antigen (PAI-1) (p<0.012) and tissue plasminogen activator (tPA) antigen levels in the oral group (p<0.002). Prothrombin fragment 1.2 and activated protein C (APC) resistance were not affected by either treatment. Transdermal HT has a less marked effect on coagulation than an equivalent oral preparation. Randomised trials are required to investigate whether this translates into less risk of cardiovascular and thromboembolic disease.
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Sugunamma, Kallu, and Dr U. Mohan Kumar. "Formulation, development and evaluation of meclizine HCL transdermal patches." Future Journal of Pharmaceuticals and Health Sciences 5, no. 3 (2025): 1–12. https://doi.org/10.26452/fjphs.v5i3.770.
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This work used a solvent evaporation approach with polyethylene glycol (PEG 400) as a plasticizer to develop a transdermal patch with meclizine Hcl using varying ratios of hydrophilic and hydrophobic polymeric systems. FT-IR spectroscopy research was used to examine the drug's and the polymers' physicochemical compatibility. The physicochemical characteristics, skin irritation, in vitro drug release, ex-vivo permeation investigations across rat abdomen skin, and stability studies of the developed patches were assessed. The medication and the polymers utilised did not interact, according to the findings of FT-IR investigations. The physicochemical parameters of each formulation were consistent. Franz diffusion cells were used to conduct in vitro permeation tests of the formulations. Formulation F3 adhered to Fick's diffusion process and demonstrated superior penetration through rat skin (8527.5±1.25µg/cm2 /hr) in comparison to the other formulations. Formulation F3, which contains the polymeric blend 19:1 Hydroxypropylmethyl Cellulose (HPMC E 50cps: Eudragit RL 100), has demonstrated optimal release when compared to other formulations and demonstrated high physical stability based on in-vitro drug release and ex-vivo skin penetration performance. Further in-vivo tests were necessary, although it has been shown that meclizine Hcl can be constructed as a matrix type transdermal drug delivery system (TDDS).
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Latif, Muhammad Shahid, Fatemah F. Al-Harbi, Asif Nawaz, et al. "Formulation and Evaluation of Hydrophilic Polymer Based Methotrexate Patches: In Vitro and In Vivo Characterization." Polymers 14, no. 7 (2022): 1310. http://dx.doi.org/10.3390/polym14071310.
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This study attempted to develop and evaluate controlled-release matrix-type transdermal patches with different ratios of hydrophilic polymers (sodium carboxymethylcellulose and hydroxypropyl methylcellulose) for the local delivery of methotrexate. Transdermal patches were formulated by employing a solvent casting technique using blends of sodium carboxymethylcellulose (CMC-Na) and hydroxypropylmethylcellulose (HPMC) polymers as rate-controlling agents. The F1 formulated patch served as the control formulation with a 1:1 polymer concentration. The F9 formulation served as our optimized formulation due to suitable physicochemical properties yielded through the combination of CMC-Na and HPMC (5:1). Drug excipient compatibilities (ATR-FTIR) were performed as a preformulation study. The ATR-FTIR study depicted great compatibility between the drug and the polymers. Physicochemical parameters, kinetic modeling, in vitro drug release, ex vivo drug permeation, skin drug retention, and in vivo studies were also carried out for the formulated patches. The formulated patches exhibited a clear, smooth, elastic nature with good weight uniformity, % moisture uptake, drug content, and thickness. Physicochemical characterization revealed folding endurance ranging from 62 ± 2.21 to 78 ± 1.54, tensile strength from 9.42 ± 0.52 to 12.32 ± 0.72, % swelling index from 37.16 ± 0.17 to 76.24 ± 1.37, and % drug content from 93.57 ± 5.34 to 98.19 ± 1.56. An increase in the concentration of the CMC-Na polymer (F9) resulted in increased drug release from the formulated transdermal patches. Similarly, drug permeation and retention were found to be higher in the F9 formulation compared to the other formulations (F1–F8). A drug retention analysis revealed that the F9 formulation exhibited 13.43% drug retention in the deep layers of the skin compared to other formulations (F1–F8). The stability study indicated that, during the study period of 60 days, no significant changes in the drug content and physical characteristics were found. ATR-FTIR analysis of rabbit skin samples treated with the formulated transdermal patches revealed that hydrophilic polymers mainly affect the skin proteins (ceramide and keratins). A pharmacokinetic profile revealed Cmax was 1.77.38 ng/mL, Tmax was 12 h, and t1/2 was 17.3 ± 2.21. In vivo studies showed that the skin drug retention of F9 was higher compared to the drug solution. These findings reinforce that methotrexate-based patches can possibly be used for the management of psoriasis. This study can reasonably conclude that methotrexate transdermal matrix-type patches with CMC-Na and HPMC polymers at different concentrations effectively sustain drug release with prime permeation profiles and better bioavailability. Therefore, these formulated patches can be employed for the potential management of topical diseases, such as psoriasis.
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Agrawal, Shyam Sunder, and Jatin Kumar Pruthi. "Development and evaluation of matrix type transdermal patch of ethinylestradiol and medroxyprogesterone acetate for anti-implantation activity in female Wistar rats." Contraception 84, no. 5 (2011): 533–38. http://dx.doi.org/10.1016/j.contraception.2011.03.005.
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Chiramala, Likhitha K.Kishore Dr. Gampa Vijay Kumar. "FORMULATION AND INVITRO EVALUATION OF GALANTAMINE PATCHES FOR TRANSDERMAL DRUG DELIVERY SYSTEM." INDO AMERICAN JOURNAL OF PHARMACEUTICAL SCIENCES 05, no. 12 (2018): 16576–82. https://doi.org/10.5281/zenodo.2429579.
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<em>In present study transdermal drug delivery of Galantamine was developed to overcome the first pass metabolism and to reduce frequency of dosing compared to oral route. Matrix type of transdermal patches were developed by using polymers Eudragit-L100, HPMCk<sub>4</sub>M and HPMCk15M.Transdermal patches were prepared by employing solvent casting method. Propylene glycol and Tween80 were selected as permeation enhancer and plasticizer. Formulations were prepared by taking </em><em>Eudragit-L100, HPMCk<sub>4</sub>M, HPMCk<sub>15</sub>M as</em><em> polymers in the concentrations of 100 mg,150 mg and 200 mg from F1-F9 formulations, </em><em>Eudragit-L100 100mg and HPMCk<sub>4</sub>M 100mg in F10</em><em>, </em><em>Eudragit-L100 100mg and HPMCk<sub>15</sub>M 100mg in F11, HPMCk<sub>4</sub>M 100mg </em><em>and </em><em>HPMCk<sub>15</sub>M 100mg in F12,</em><em> all the formulations were evaluated for various physical parameters, invitro drug release studies by using dialysis membrane. Among all the formulations F6 formulation was found to be best and shown 96.5% drug release in 12 hours. For F6 formulation release kinetics were applied and it was observed that the formulation was following peppas mechanism of drug release. Drug excipient compatibility studies were carried out by using FTIR, and it was observed that they were no interactions.</em> <strong>Keywords: </strong><em>Galantamine , Transdermal patch, Eudragit-L100, HPMCk<sub>4</sub>M and HPMCk15M</em>