Journal articles: 'Sustained release profile'

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Pradeep Kumar, M., Goparaju Suryanarayana Murthy, Annamdasu Lakshmi Poojitha, P. Sindhuri, A. Sreekanth, and Yerikala Ramesh. "Formulation and Evaluation of Colchicine Sustained release tablet by using factorial designs." Journal of Drug Delivery and Therapeutics 11, no. 5-S (October 26, 2021): 100–107. http://dx.doi.org/10.22270/jddt.v11i5-s.5028.

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The study on the effect of polymer concentration on in vitro drug release profile revealed that there is a change in vitro drug release parameters (t50, t80, and MDT) with a change in polymer concentration. Fraction of HPMC K4M, HPMC K 100 M, and Ethyl Cellulose were required to be 15, 10, and 7 mg respectively for designing optimized batch F7. The release rate of Colchicine decreased proportionally with an increase in the concentration of ethyl Cellulose and HPMC K100 M. Also the high amount of HPMC K4M leads to the less initial release and sustain effect. A theoretical drug release profile was generated using pharmacokinetic parameters of Colchicine. The value of t50 and t80 of theoretical drug release profile was found to be 242 min and 529 min respectively. The similarity factor f2 was applied between the in vitro drug release profile of optimizing batches and theoretical profile, which indicate a decent similarity between all in vitro drug release profiles (f2 = 68.28 for F7). All the batches except F1shows the value of f2 value within a range. Batch F7 showed the highest f2 (f2 = 68.28) among all the batches and this similarity was also reflected in t50 (≈ 256 min) and t80 (≈ 554 min) values. A 23 full factorial design was applied to systemically optimize in vitro drug release profile. The HPMC K4M (X1), Concentration of HPMC K100 M (X2), and concentration of EC (X3) were selected as independent variables. The time required for 50% drug released (t50), the time required for 80% drug release (t80), similarity factor f2, and mean dissolution time (MDT) were selected as dependent variables. The results of full factorial design indicate that the HPMC K4M (X1), Concentration of HPMC K100 M (X2), and concentration of EC (X3) have a significant effect on in vitro drug release profile. To find out the release mechanism the in vitro release data were fitted in the Korsmeyer-Peppas equation. All Batches except F1 and F3 show Anomalous diffusion-controlled release (combined mechanism of diffusion and case II transport).

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Schattenkirchner, M. "The safety profile of sustained-release etodolac." Rheumatology International 13, S2 (June 1993): S31—S35. http://dx.doi.org/10.1007/bf00290282.

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Thanh, Duyen Nguyen Thi, Duc Hoang Van, Minh Vo Xuan, Xuan Dam Thanh Thanh, and Tung Bui Thanh. "Design and Optimization of Hydrophilic Matrix-based Sustained Release Felodipine Tablets." International Journal of Pharmaceutical Sciences and Nanotechnology 11, no. 3 (May 31, 2018): 4136–44. http://dx.doi.org/10.37285/ijpsn.2018.11.3.8.

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Felodipine is a calcium channel blocker used for hypertensive and unstable angina treatments. The sustained release formulations of felodipine have advantages of achieving good therapeutic effects, increasing the bioavailability, decreasing dosing times per day and reducing side effects.The aim of our study was to study the formulation screening, then use an experiment design for formulating a hydrophilic matrix sustained release tablet of felodipine. Methods: The optimization process had the influences of the chosen excipients (including HPMC E4M, HPMC E15LV) on the drug release. Three dependent variables were percentages of released felodipine at the sampling times 2h, 6h, 10h (Y2, Y6, Y10, respectively). Results: The release profile from the optimized formula almost met the predicted release profile and was similar to reference tablets. The kinetics of drug release the optimized tablets and reference tablets were also followed the Korsmeyer – Peppas model.Conclusion: The optimized formula was obtained, and the in vitro release profile was similar to the predicted profile and reference tablets.

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Jenner, Adrianne L., Federico Frascoli, Chae-Ok Yun, and Peter S. Kim. "Optimising Hydrogel Release Profiles for Viro-Immunotherapy Using Oncolytic Adenovirus Expressing IL-12 and GM-CSF with Immature Dendritic Cells." Applied Sciences 10, no. 8 (April 21, 2020): 2872. http://dx.doi.org/10.3390/app10082872.

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Sustained-release delivery systems, such as hydrogels, significantly improve cancer therapies by extending the treatment efficacy and avoiding excess wash-out. Combined virotherapy and immunotherapy (viro-immunotherapy) is naturally improved by these sustained-release systems, as it relies on the continual stimulation of the antitumour immune response. In this article, we consider a previously developed viro-immunotherapy treatment where oncolytic viruses that are genetically engineered to infect and lyse cancer cells are loaded onto hydrogels with immature dendritic cells (DCs). The time-dependent release of virus and immune cells results in a prolonged cancer cell killing from both the virus and activated immune cells. Although effective, a major challenge is optimising the release profile of the virus and immature DCs from the gel so as to obtain a minimum tumour size. Using a system of ordinary differential equations calibrated to experimental results, we undertake a novel numerical investigation of different gel-release profiles to determine the optimal release profile for this viro-immunotherapy. Using a data-calibrated mathematical model, we show that if the virus is released rapidly within the first few days and the DCs are released for two weeks, the tumour burden can be significantly decreased. We then find the true optimal gel-release kinetics using a genetic algorithm and suggest that complex profiles present unnecessary risk and that a simple linear-release model is optimal. In this work, insight is provided into a fundamental problem in the growing field of sustained-delivery systems using mathematical modelling and analysis.

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Khoder, Mouhamad, Henry Gbormoi, Ali Ryan, Ayman Karam, and Raid Alany. "Potential Use of the Maillard Reaction for Pharmaceutical Applications: Gastric and Intestinal Controlled Release Alginate-Albumin Beads." Pharmaceutics 11, no. 2 (February 15, 2019): 83. http://dx.doi.org/10.3390/pharmaceutics11020083.

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In this study, bovine serum albumin (BSA) and alginate (ALG) conjugates were synthesized by the Maillard reaction in order to evaluate their potential to develop controlled release drug delivery systems. The progress of the Maillard reaction was evidenced using ultraviolet (UV) absorbance, determination of BSA remaining free amino groups, and sodium dodecyl sulfate polyacrylamide gel electrophoresis (SDS-PAGE). BSA-ALG conjugates possessed enhanced and tunable viscosity, foamability and foam stability. Foam generated from BSA-ALG conjugate solution was used to prepare floating gastroretentive calcium ALG beads. Unlike traditional ALG beads, BSA-ALG foam beads were able to float and sustain the ciprofloxacin (CIP) release in gastric medium. Interestingly, intestinal beads made of ALG, BSA-ALG physical mixture and BSA-ALG conjugate resulted in different release rates and orders of indomethacin (IND) in simulated intestinal fluids; while beads based on a physical mixture of BSA-ALG resulted in a first order sustained release profile, both systems based on ALG and BSA-ALG conjugate displayed zero order sustained release profiles with IND being released at a slower rate from the conjugate beads.

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Jungnickel, Paul W., and Pierre A. Maloley. "Comment: Adverse-Effect Profile of Sustained-Release Niacin." DICP 25, no. 9 (September 1991): 1014. http://dx.doi.org/10.1177/106002809102500925.

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Rahman, Md Ziaur, Sayed Koushik Ahamed, Sujan Banik, and Mohammad Salim Hossain. "Release Profile of Losartan Potassium from Formulated Sustained Release Matrix Tablet." Bangladesh Pharmaceutical Journal 16, no. 2 (February 20, 2015): 177–83. http://dx.doi.org/10.3329/bpj.v16i2.22301.

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The present study was undertaken to develop sustained release (SR) matrix tablets of Losartan potassium, an angiotensin-II antagonist for the treatment of hypertension. The tablets were prepared by direct compression method along with Kollidon SR and Methyl Cellulose as release retardant polymers. The evaluation involves two stages- the physical properties studies of tablets and in vitro release kinetics assessment. The USP paddle method was selected to perform the dissolution test and 900 ml phosphate buffer of pH 6.8 was used as dissolution medium at 50 rpm at 370C. The release kinetics were analyzed. All the formulations followed Higuchi release kinetics. When the release data was plotted into Korsmeyer-Peppas equation, then it was confirmed that F-1, F-2, F-3, F-4 and F-5 exhibited non-fickian type drug release whereas F-6 exhibited fickian type drug release from the tablet matrix. The in-vitro release studies revealed that the formulation F-2 can be taken as an ideal or optimized formulation of sustained release tablets for 24 hours release as it fulfills all the requirements for sustained release tablet. Furthermore, when the tablets were preheated at different temperature (300C, 450C, 600C) before dissolution they showed decrease in drug release compared with ambient temperature DOI: http://dx.doi.org/10.3329/bpj.v16i2.22301 Bangladesh Pharmaceutical Journal 16(2): 177-183, 2013

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Mishra, DinaNath, Kalpana Nagpal, ShailendraKumar Singh, and Vikas Mathur. "Comparative release profile of sustained release matrix tablets of verapamil HCl." International Journal of Pharmaceutical Investigation 3, no. 1 (2013): 60. http://dx.doi.org/10.4103/2230-973x.108965.

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Dharmayanti, Cintya, Todd A. Gillam, Desmond B. Williams, and Anton Blencowe. "Drug-Eluting Biodegradable Implants for the Sustained Release of Bisphosphonates." Polymers 12, no. 12 (December 7, 2020): 2930. http://dx.doi.org/10.3390/polym12122930.

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Despite being one of the first-line treatments for osteoporosis, the bisphosphonate drug class exhibits an extremely low oral bioavailability (<1%) due to poor absorption from the gastrointestinal tract. To overcome this, and to explore the potential for sustained drug release, bioerodible poly(lactic acid) (PLA) and poly(D,L-lactide-co-glycolide) (PLGA) implants loaded with the bisphosphonate alendronate sodium (ALN) were prepared via hot-melt extrusion. The rate of drug release in vitro was modulated by tailoring the ratio of lactide to glycolide in the polymer and by altering the ALN-loading of the implants. All investigated implants exhibited sustained ALN release in vitro between 25 to 130 days, where implants of greater glycolide composition and higher ALN-loadings released ALN more rapidly. All PLGA implants demonstrated a sigmoidal release profile, characterised by an initial surface dissolution phase, followed by a period of zero-order drug diffusion, then relaxation or erosion of the polymer chains that caused accelerated release over the subsequent days. Contrastingly, the PLA implants demonstrated a logarithmic release profile, characterised by a gradual decrease in ALN release over time.

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Li, Xiao Yan, Deng Guang Yu, Fa Ping Jiang, Kong Jing Deng, Zhi Du, and Xia Wang. "Drug Sustained Release Multiple-Component Polymeric Microparticles Fabricated Using an Electrospray Process." Advanced Materials Research 937 (May 2014): 269–75. http://dx.doi.org/10.4028/www.scientific.net/amr.937.269.

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The present study investigates the preparation of ferulic acid (FA) sustained-release cellulose acetate (CA) microparticles, in which a third component, polyvinylpyrrolidone (PVP), was included into the microcomposites for an improved sustained drug release profile. An electrospraying process was exploited for the fabrication of multiple-component microparticles. Under an applied voltage of 18 kV, FA/PVP/CA composite microparticles were successfully generated. Field emission scanning electron microscopic observations demonstrated that these microparticles had an indented surface morphology with an average diameter of 1.71 ± 0.56 μm. The drug presented in the polymeric microparticles in an amorphous state due to the favorable secondary interactions among the components, as verified by the X-ray diffraction (XRD) patterns and attenuated total reflectance Fourier transform spectra. The triple-component microparticles could provide a fine sustained release profiles with full release completeness and small tailing-off release time period. The electrospraying process is a useful tool for developing sustained release microparticles and multiple-component co-existence in the microparticles can be taken to adjust the sustained drug release profiles.

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Alshetaili, Abdullah, Bjad K. Almutairy, Sultan M. Alshehri, and Michael A. Repka. "Development and Characterization of Sustained-Released Donepezil Hydrochloride Solid Dispersions Using Hot Melt Extrusion Technology." Pharmaceutics 13, no. 2 (February 4, 2021): 213. http://dx.doi.org/10.3390/pharmaceutics13020213.

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The aim of this work was to develop the sustained release formulation of donepezil hydrochloride (DH) using the hot-melt extruded solid dispersion technique via the rational screening of hydrophobic carriers. Hydrophobic carriers with different physicochemical properties such as pH-independent swellability, low-permeability (Eudragit® RS PO (E-RS)), pH-independent non-swellability (ethyl cellulose N7 (EC-N7)), and the presence of lipids (Compritol® 888 ATO (C-888)) with or without pore-forming agents were used to achieve the sustained release profile of DH. Mannitol (MNT) was chosen as the temporary pore-forming agent. The thermal analysis showed that both the drug and C-888 preserved their crystallinity within a solid dispersion. During a dissolution test, MNT could generate pores, and the drug release rate was proportionally correlated to the MNT content. Tailoring of the ratio of C-888 and MNT in the formulations along with an appropriate extrusion temperature profile resulted in the modified release of DH, and a preferable release pattern was obtained under these conditions. C-888 was chosen for the further investigations to obtain tablets with a high integrity. The optimized tablets were compared to the marketed formulation of Aricept® in terms of drug release profiles. The optimized formulation showed the stable and sustained release behavior of extended release profile, which was close to the release behavior of Aricept® with good tablet characteristics. It was concluded that the hot-melt extrusion technique can be utilized for the manufacturing of DH sustained release tablets with improved tablet integrity and characteristics by co-processing the tablet excipient with DH/C-888.

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Patel, Sulabh P., Ravi Vaishya, Gyan Prakash Mishra, Viral Tamboli, Dhananjay Pal, and Ashim K. Mitra. "Tailor-Made Pentablock Copolymer Based Formulation for Sustained Ocular Delivery of Protein Therapeutics." Journal of Drug Delivery 2014 (June 22, 2014): 1–15. http://dx.doi.org/10.1155/2014/401747.

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The objective of this research article is to report the synthesis and evaluation of novel pentablock copolymers for controlled delivery of macromolecules in the treatment of posterior segment diseases. Novel biodegradable PB copolymers were synthesized by sequential ring-opening polymerization. Various ratios and molecular weights of each block (polyglycolic acid, polyethylene glycol, polylactic acid, and polycaprolactone) were selected for synthesis and to optimize release profile of FITC-BSA, IgG, and bevacizumab from nanoparticles (NPs) and thermosensitive gel. NPs were characterized for particle size, polydispersity, entrapment efficiency, and drug loading. In vitro release study of proteins from NPs alone and composite formulation (NPs suspended in thermosensitive gel) was performed. Composite formulations demonstrated no or negligible burst release with continuous near zero-order release in contrast to NPs alone. Hydrodynamic diameter of protein therapeutics and hydrophobicity of PB copolymer exhibited significant effect on entrapment efficiency and in vitro release profile. CD spectroscopy confirmed retention of structural conformation of released protein. Biological activity of released bevacizumab was confirmed by in vitro cell proliferation and cell migration assays. It can be concluded that novel PB polymers can serve a platform for sustained delivery of therapeutic proteins.

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Karim, Samira, Mohiuddin Ahmed Bhuiyan, and Md Sohel Rana. "Formulation and in vitro Evaluation of Glimepiride Sustained Release Tablets: Comparison with Immediate Release Tablets." Bangladesh Pharmaceutical Journal 18, no. 2 (July 26, 2015): 157–62. http://dx.doi.org/10.3329/bpj.v18i2.24315.

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This work aims at the design of a sustained release formulation of glimepiride which is currently available in the treatment of type 2 diabetes mellitus and to investigate the effect of polymers on the release profile of glimepiride. Glimepiride sustained release tablets were prepared by direct compression method using different ratios of various release retarding polymers such as carbopol, ethyl cellulose, methocel K4 MCR, methocel K15 MCR, methocel K100 MCR and xanthum gum. These formulations were also compared with glimepiride immediate release tablets. The prepared tablets were subjected to various physical parameter tests including weight variation, friability, hardness, thickness, diameter, etc. In vitro dissolution studies of the formulations were done at pH 6.8 in phosphate buffer using USP apparatus 2 (paddle method) at 50 rpm. The percent releases of all the formulations (30) were 73.11%- 98.76% after 8 hours. The release pattern followed zero order kinetics and the release of the drug was hindered by the polymers used in the study. On the other hand, 100% drug was released within 1 hour from the immediate release tablet of glimepiride. The study reveals that the polymers used have the capacity to retard the release of the drug from the sustained release tablets and the more is the amount of the polymer in the formulation the less is the release of drug showing more retardation of drug release.Bangladesh Pharmaceutical Journal 18(2): 157-162, 2015

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Senthilvel, Chitra Karthikeyini, Kavitha Karuppaiyan, Ananth Pothumani, Ananthi Vedharethinam, Ancy Wilfred Jose, Jamal Moideen Muthu Mohamed, Mohamed El Sherbiny, Hasnaa Ali Ebrahim, Mohamed El Shafey, and Minilu Dejene. "Development of Atorvastatin Calcium Biloaded Capsules for Oral Administration of Hypercholesterolemia." Evidence-Based Complementary and Alternative Medicine 2022 (May 16, 2022): 1–11. http://dx.doi.org/10.1155/2022/4995508.

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The goal of this study was to develop atorvastatin (ATN) calcium biloaded, i.e., immediate release (IR) and sustained release (SR) capsules that would promote the quick onset of action and a better dissolution profile on both the IR and SR aspects. The IR granules were prepared by the wet granulation method, and an aqueous solubility study proved that the IR granules released the ATN within 25 min compared to the pure drug due to the addition of PEG and super disintegrants such as croscarmellose (CC) and crospovidone (CP). The sustained release nanoparticles (SR-NPs) were synthesized using a solvent evaporation technique and an optimal combination of hydrophilic and hydrophobic polymers. The addition of a hydrophobic polymer to a hydrophilic polymer delays drug release, resulting in a sustained and controlled release lasting up to 12 hours. The drug release of ATN from SR nanoparticles followed the Higuchi and Korsmeyer–Peppas models and had first-order kinetics (r2 = ???). Fourier transform infrared spectrophotometry, powder X-ray diffraction, and differential scanning calorimetric analysis were used to test the prepared biloaded capsules, and the results showed that there was no significant interaction between the polymers, excipients, and drug. The SEM and DLS analysis clearly demonstrated that drug particles in a continuous layer were enclosed by polymers at the nanoscale. To summarise, integrating both layers into a single capsule resulted in a superior release profile and patient compliance. Finally, prepared biloaded capsules were discovered to exhibit both an IR and an SR profile.

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Junyaprasert, Varaporn Buraphacheep, and Greepol Manwiwattanakul. "Release profile comparison and stability of diltiazem–resin microcapsules in sustained release suspensions." International Journal of Pharmaceutics 352, no. 1-2 (March 2008): 81–91. http://dx.doi.org/10.1016/j.ijpharm.2007.10.018.

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Yang, Shuoye. "Preparation and evaluation of novel galantamine hydrobromide sustained-release capsule." Bangladesh Journal of Pharmacology 11 (March 5, 2016): S82—S91. http://dx.doi.org/10.3329/bjp.v11is1.26417.

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In present study, a novel galantamine hydrobromide sustained-release capsule was prepared with the extrusion-spheronization method and the optimized preparative formulation. The release studies were performed using marketed capsules (Razadyne ER) as a reference and data were analyzed in terms of cumulative release amounts as a function of time. Furthermore, fiber-optic real time detection was adopted to monitor the release process. Results demonstrated that our developed formulation had superior properties, worked better as sustained-release carriers and lasted longer time to release compared with the marketed product. The in vitro release characteristics of different batches of preparations were quite similar with each other, the total release proportions of galantamine hydrobromide from sustained-release capsules reached higher than 90% within 12 hours. Similar factors f2 of two preparations were all higher than 50, the release profile of drugs from capsules fitted to Higuchi model with the equation of Q% = 0.2681t1/2 + 0.0684 (r = 0.9966). Pharmacokinetics profile and parameters in beagle dogs after oral administration also revealed the superior release performances of new capsules being consistent with the in vitro study. The developed sustained-release formulation may be a promising alternative dosage form for treatment of related diseases.

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Damien, Gerard, Bruno Huet de Barochez, and Pierre Schiavi. "Galenic Development and Pharmacokinetic Profile of Indapamide Sustained Release 1.5mg." Clinical Pharmacokinetics 37, Supplement 1 (1999): 13–19. http://dx.doi.org/10.2165/00003088-199937001-00003.

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Weidmann, Peter. "Metabolic Profile of Indapamide Sustained-Release in Patients with Hypertension." Drug Safety 24, no. 15 (2001): 1155–65. http://dx.doi.org/10.2165/00002018-200124150-00006.

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Resch, H., C. Libanati, J. Talbot, M. Tabuenca, S. Farley, P. Bettica, W. Tritthart, and D. Baylink. "Pharmacokinetic profile of a new fluoride preparation: Sustained-release monofluorophosphate." Calcified Tissue International 54, no. 1 (January 1994): 7–11. http://dx.doi.org/10.1007/bf00316281.

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Gavan, Alexandru, Alina Porfire, Cristina Marina, and Ioan Tomuta. "Formulation and pharmaceutical development of quetiapine fumarate sustained release matrix tablets using a QbD approach." Acta Pharmaceutica 67, no. 1 (March 1, 2017): 53–70. http://dx.doi.org/10.1515/acph-2017-0009.

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AbstractThe main objective of the present study was to apply QbD methodology in the development of once-a-day sustained release quetiapine tablets. The quality target product profile (QTPP) was defined after the pharmaceutical properties and kinetic release of the innovator product, Seroquel XR 200 mg. For the D-optimal experimental design, the level and ratio of matrix forming agents and the type of extragranular diluent were chosen as independent inputs, which represented critical formulation factors. The critical quality attributes (CQAs) studied were the cumulative percentages of quetiapine released after certain time intervals. After the analysis of the experimental design, optimal formulas and the design space were defined. Optimal formulas demonstrated zero-order release kinetics and a dissolution profile similar to the innovator product, with f2values of 74.53 and 83.74. It was concluded that the QbD approach allowed fast development of sustained release tablets with similar dissolution behavior as the innovator product.

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Mawazi, Al-Mahmood, Chatterjee, Hadi, and Doolaanea. "Carbamazepine Gel Formulation as a Sustained Release Epilepsy Medication for Pediatric Use." Pharmaceutics 11, no. 10 (September 20, 2019): 488. http://dx.doi.org/10.3390/pharmaceutics11100488.

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This study aimed to develop a carbamazepine (CBZ) sustained release formulation suitable for pediatric use with a lower risk of precipitation. The CBZ was first prepared as sustained release microparticles, and then the microparticles were embedded in alginate beads, and finally, the beads were suspended in a gel vehicle. The microparticles were prepared by a solvent evaporation method utilizing ethyl cellulose as a sustained release polymer and were evaluated for particle size, encapsulation efficiency, and release profile. The beads were fabricated by the dropwise addition of sodium alginate in calcium chloride solution and characterized for size, shape, and release properties. The gel was prepared using iota carrageenan as the gelling agent and evaluated for appearance, syneresis, drug content uniformity, rheology, release profile, and stability. The microparticles exhibited a particle size of 135.01 ± 0.61 µm with a monodisperse distribution and an encapsulation efficiency of 83.89 ± 3.98%. The beads were monodispersed with an average size of 1.4 ± 0.05 mm and a sphericity factor of less than 0.05. The gel was prepared using a 1:1 ratio (gel vehicle to beads) and exhibited no syneresis, good homogeneity, and good shear-thinning properties. The release profile from the beads and from the gel was not significantly affected, maintaining similarity to the tablet form. The gel properties were maintained for one month real time stability, but the accelerated stability showed reduced viscosity and pH with time. In conclusion, CBZ in a gel sustained release dosage form combines the advantages of the suspension form in terms of dosing flexibility, and the advantages of the tablet form in regards to the sustained release profile. This dosage form should be further investigated in vivo in animal models before being considered in clinical trials.

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Yu, Deng Guang, Wei Qian, Xia Wang, Ying Li, Wei Jun Lu, and Yong Zhang. "Ferulic Acid-Loaded Shellac Microparticles Prepared Using Electrohydrodynamic Atomization." Advanced Materials Research 675 (March 2013): 326–30. http://dx.doi.org/10.4028/www.scientific.net/amr.675.326.

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An Electrohydrodynamic atomization (EHDA) process was exploited to prepare ferulic acid (FA)-loaded shellac microparticles. SEM observations showed that all the particles were round and solid with their sizes gradually increased from 0.68 ± 0.21 to 2.75 ± 0.64 μm as the concentrations of shellac and FA in ethanol raised from 20% to 50% (w/v). Wide-angle X-ray diffraction analyses demonstrated that FA had been totally converted into an amorphous state in the shellac matrix microparticles. Attenuated total reflectance Fourier transform infrared analysis disclosed that the hydrogen bonding presented between FA and shellac molecules. In vitro dissolution tests verified that all the microparticles were able to provide a fine sustained drug release profile. The release time periods had a close relationship with the diameters of microparticles. All the microparticles released the loaded FA via a typical Fickian diffusion mechanism. The present study provides an easy way to develop novel drug delivery microparticles for providing sustained drug release profiles.

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Lin, Esther Marie JieRong, Chee Leng Lay, Gomathy Sandhya Subramanian, Wui Siew Tan, Susanna Su Jan Leong, Lionel Chuan Hui Moh, and Kaiyang Lim. "Control Release Coating for Urinary Catheters with Enhanced Released Profile for Sustained Antimicrobial Protection." ACS Applied Materials & Interfaces 13, no. 49 (November 30, 2021): 59263–74. http://dx.doi.org/10.1021/acsami.1c17697.

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Viswanath, V., U. Chandrasekhar, B. Narasimha Rao, and K. Gnana Prakash. "Development and evaluation of sustained release matrix tablets of losartan potassium." INTERNATIONAL JOURNAL OF APPLIED PHARMACEUTICAL SCIENCES AND RESEARCH 1, no. 04 (December 6, 2016): 127–32. http://dx.doi.org/10.21477/ijapsr.v3i1.4858.

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The objective of the present study was to develop a sustained release matrix tablets of Losartan potassium, an anti hypertensive drug. The sustained release tablets were prepared by wet granulation and formulated using different drug and polymer ratios. Hydrophilic natural polymers like xanthan Gum (XG), guar gum and cellulose were used. Compatibility of the drug with various excipients was studied. The compressed tablets were evaluated and showed compliance with Pharmacopoeial limits. Formulation was optimized (F2) on the basis of acceptable tablet properties and in vitro drug release. The resulting formulation produced matrix tablets with optimum hardness, consistent weight uniformity and friability. All tablets but one exhibited gradual and near completion sustained release for losartan potassium and 90.88% released at the end of 12h. The results of dissolution studies indicated that formulation F2 (drug to polymer 1:2) is the most successful of the study and exhibited drug release pattern very close to theoretical release profile. A decrease in release kinetics of the drug was observed on increasing polymer ratio. Applying exponential equation, all the formulation tablets (except F2) showed diffusion-dominated drug release. The mechanism of drug release from F2 was diffusion coupled with erosion.

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Patel, Dhaval M., Riddhi Trivedi, and Hardik Patel. "Formulation and Evaluation of Bi-Layer Tablets of Ketorolac Tromethamine." Journal of Drug Delivery and Therapeutics 11, no. 1 (January 15, 2021): 36–41. http://dx.doi.org/10.22270/jddt.v11i1.4487.

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The objective of the present study was to develop and evaluate bi-layer tablets of Ketorolac tromethamine, a nonsteroidal antiinflammatory drug with short half-life, that are characterized by initial burst drug release in the stomach and comply with the release requirements of sustained-release products. Each of the proposed bi-layer tablets is composed of an immediate-release layer and a sustained-release layer, anticipating rapid drug release that starts in the stomach to rapidly alleviate the symptoms and continues in the intestine to maintain protracted analgesic effect. Gastro retentive Bi-Layer tablets of Ketorolac Tromethamine were prepared by using hydrophilic polymers with direct compression on floating – matrix technology and evaluated. Ketorolac tromethamine is freely soluble in water, so it is suitable to develop it as gastro retentive bi-layer tablets using hydrophilic polymers. The developed formulation is equivalent to calculated theoretical drug profile in view of its in vitro release. Immediate release layer was prepared by using dry granulation method in which ac-di sol used as a disintigrant for immediate release of drug. Sustained release layer formulated by using HPMC as release retardant, two grades of HPMC that are HPMC K4M and HPMC K100M used to get sustained release profile for 24 hr. Various trial batches are taken to get desired release profile. Ketorolac tromethamine release from the developed floating formulation followed Higuchi model and nonFickian diffusion is found to be the main mechanism of drug release. The manufacturing procedure was found to be reproducible and formulations were stable after one month of stability studies. Keywords: FTIR; Gastro retentive bilayer; ketorolac tromethamine; in vitro release; stability; higuchi.

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Shin, Yu Na, Mi Hee Cho, Hyun Hee Ahn, Moon Suk Kim, Gil Son Ghang, and Hai Bang Lee. "Preparation and Release Profile of BDNF-Loaded PLGA/SIS Scaffold." Key Engineering Materials 342-343 (July 2007): 413–16. http://dx.doi.org/10.4028/www.scientific.net/kem.342-343.413.

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The goal of this study was to investigate release tendency of brain-derived neurotrophic factor (BDNF) from poly(L-lactide-co-glycolide) (PLGA) and small intestine submucosa (SIS) scaffold prepared by ice-leaching method. A porous scaffold consisting of PLGA and SIS as carrier of BDNF has been prepared in the presence of ice particle. SEM image of the PLGA/SIS scaffold showed an interconnected pore structure. The release behavior of BDNF loaded PLGA/SIS scaffold was examined for 4 weeks period at phosphate buffered saline (PBS, pH 7.4) at 37 oC. The sustained release of BDNF over 4 weeks was observed from the PLGA/SIS scaffold. These results indicate that the sustained release of BDNF from PLGA/SIS scaffold can be very useful for application in the tissue engineering.

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Tambare, Rashmi Shivaji, Ganesh G. Tapadiya, and Sadhana R. Shahi. "Formulation and Evaluation of Controlled Release Matrix Tablets of Cefixime Trihydrate." Middle East Research Journal of Pharmaceutical Sciences 1, no. 1 (December 30, 2021): 38–44. http://dx.doi.org/10.36348/merjps.2021.v01i01.005.

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Abstract: The main objective of the present work was to develop sustained release matrix tablets of Cefixime Trihydrate were prepared by direct compression techniques and evaluates the effect of formulation variables such as lubricant, binder, polymer content and viscosity grades of HPMC on the behavior of Cefixime Trihydrate release. The prepared tablets were evaluated for various physico-chemical parameters. In vitro release profile was check to evaluate the sustained release matrix tablet of Cefixime Trihydrate. The drug release from the optimized formulation was found to follow zero order kinetics. Thus the phenomenon of drug release showed that the release of optimized formulation is controlled by diffusion. Administration of Cefixime Trihydrate in a sustained release dosage would be more desirable for bacterial infections effects by maintaining the plasma concentrations of the drug well above the therapeutic concentration. From In vitro dissolution profile, Formulation S3 was prepared with Hydroxypropyl methylcellulose (K15M) combination where drug release was about 99.14% at the end of 24 hrs and followed zero order with non-Fickian diffusion method. It is selected as the best formulation.

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Abdulkhaleq, Nuha Mohammed, and Mowafaq M. Ghareeb. "Combination of FDM 3D Printing and Compressed Tablet for Preparation of Baclofen as Gastro-Floating Drug Delivery System (Conference Paper )#." Iraqi Journal of Pharmaceutical Sciences ( P-ISSN 1683 - 3597 E-ISSN 2521 - 3512) 31, Suppl. (February 16, 2023): 18–24. http://dx.doi.org/10.31351/vol31isssuppl.pp18-24.

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This study aimed to develop an oral drug delivery system for gastro-retentive sustained drug release of baclofen by using a 3D printed capsular device since baclofen has a short half-life of 2.5 to 4 hours and has a narrow absorption window. Firstly sustained-release tablets of baclofen were formulated through the hot-melt extrusion of various thermoplastic polymers and direct compression of the extrudate, then a capsular device was designed and 3D printed to contain two air pockets to enable floating of the device and has four windows for drug release. 3D printing of the capsular device was done by an FDM printer using biodegradable PLA filament, and the sustained release tablets were inserted into the device to allow the medicine to be released into the stomach over a longer period. An in vitro buoyance test and an in vitro dissolution test were used to examine the buoyancy and sustained-release features of the formulated gastro-floating system. Five sustained release formulas were developed using different thermoplastic polymers in hot-melt extrusion. Produced tablets were assayed for drug content, hardness, and friability while a DSC study was done on the selected formula. F 5 which contains 20% baclofen, 55% Eudragit RS-100, 20% ethylcellulose, and 5% PEG 4000 showed sustained release where the complete dissolution of the drug occurred in 12 hours, and the gastro-floating device remained floating all the time. This method has a great potential for developing various floating drug delivery systems with the required release profile.

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Aldilla, Vina R., Adam D. Martin, Shashidhar Nizalapur, Christopher E. Marjo, Anne M. Rich, Kitty K. K. Ho, Lars M. Ittner, David StC Black, Pall Thordarson, and Naresh Kumar. "Glyoxylamide-based self-assembly hydrogels for sustained ciprofloxacin delivery." Journal of Materials Chemistry B 6, no. 38 (2018): 6089–98. http://dx.doi.org/10.1039/c8tb01290c.

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Yang, Hui, Peng Fei Gao, Wen Bi Wu, Xiao Xi Yang, Qiao Ling Zeng, Chong Li, and Cheng Zhi Huang. "Antibacterials loaded electrospun composite nanofibers: release profile and sustained antibacterial efficacy." Polym. Chem. 5, no. 6 (2014): 1965–75. http://dx.doi.org/10.1039/c3py01335a.

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Basarkar, Ganesh D., Ketan H. Shah, and Madhuri B. Sonawane. "Formulation Development and Evaluation of Sustained Release Matrix Tablets of Guaiphenesin." International Journal of Pharmaceutical Sciences and Nanotechnology 9, no. 3 (May 31, 2016): 3312–16. http://dx.doi.org/10.37285/ijpsn.2016.9.3.7.

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In this study we sought to formulate and evaluate sustained release matrix tablet of guaiphenesin by melt granulation technology. The sustained release tablets were prepared by melt granulation technique using rice bran wax as a drug retardant and dibasic calcium phosphate (DCP) as a channelling agent. Guaiphenesin is an expectorant and has a short plasma half-life of one hour. Because of high frequency of administration and short biological half-life, guaiphenesin was considered as model drug. Sustained release formulation that would maintain plasma levels for 12 hours is sufficient for twice daily dosing of guaiphenesin. The compatibility of drug and wax was examined by differential scanning calorimetry (DSC). The effect of waxes at different (drug: wax) concentrations on the release profile of drug from matrix formulation were studied. Drug release was studied at pH 1.2 for 2 hour and pH 6.8 for 10 hours. A significant retardation in the drug release was observed by increasing the wax concentration. The drug release study revealed that wax concentration of 30% to be optimum. Dissolution study showed 99% drug release within 12 hrs. Kinetic modelling of in vitro dissolution profiles revealed the drug release mechanism ranges from diffusion controlled or Fickian transport to anomalous type or non-Fickian transport. These results suggest that the rice bran wax has good release retardant property for highly water-soluble drug such as guaiphenesin.

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Kalbhare, Shankar, Rohit K. Pawar, Vivekkumar K. Redasani, Amita B. Yadav, Vishal R. Mohite, and Vaibhav B. Kadam. "Role of Aminated Derivatives of Natural Gum in Release Modulating Matrix System of Losartan Potassium." International Journal of Pharmaceutical Sciences and Nanotechnology(IJPSN) 15, no. 6 (December 12, 2022): 6204–15. http://dx.doi.org/10.37285/ijpsn.2022.15.6.3.

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Objective: The investigation aimed to synthesize amino derivatives of various natural gums like Xanthan gum and Tamarind gum for using them as a release modulating polymer in the formulation of the hydrophilic matrix system of losartan potassium and to find the best amongst them. Developing oral sustained release matrix tablets for a drug with a constant release rate has always been a challenge to the pharmaceutical technologist. Materials and Methods: Release modulating hydrophilic matrix tablets of losartan potassium were prepared by wet granulation method. A total number of 6 formulations of release modulating hydrophilic matrix tablets of losartan potassium were prepared using different polymeric ratios of Carbopol 934, aminated Tamarind gum and aminated Xanthan gum based on preliminary trial bathes. The formulated tablets were evaluated for both pre-compression and post-compression evaluation studies. Results: Based on in vitro drug release study the effective formulations AXG 3 are shows a maximum similar release profile to other remains formulations with a theoretical drug release profile of losartan potassium for sustained release. Finally optimized formulation AXG 3 containing carbopol 934 (60 mg), aminated xanthan gum (40 mg), MCC (190 mg) and magnesium stearate (10 mg) showed 100±0.024 % drug release in 12 hr which is acceptable with theoretical drug release of losartan potassium for sustain release dose. Conclusion: Aminated derivatives of xanthan gum and Tamarind gum extend the drug release for 12 hr. Based on in vitro drug release studies of formulations, we concluded that the alteration in the concentration of carbopol 934 with an aminated derivative of xanthan gum in sustain release formulation development was more effective and economical.

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Okafo, Sinodukoo E., John A. Avbunudiogba, and Ejiro Ejomafuvwe. "Formulation and evaluation of sustained release diclofenac sodium matrix tablets produced using Brachystegia eurycoma gum." Journal of Pharmacy & Bioresources 17, no. 1 (May 22, 2020): 34–43. http://dx.doi.org/10.4314/jpb.v17i1.7.

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This study was carried out to evaluate sustained release diclofenac sodium matrix tablets formulated using Brachystegia eurycoma gum (BEG) as matrix polymer. BEG was isolated by acetone -precipitation of the filtrate obtained from the maceration of powdered dried seeds of Brachystegia eurycoma in distilled water. Diclofenac sodium matrix tablets were produced by non-aqueous wet granulation method using BEG as the hydrophilic matrix former. The tablets were evaluated using official and unofficial tests such as; uniformity of weight, content uniformity, dissolution test, tablets diameter, thickness, hardness and friability tests. The drug release profile of the matrix tablets were compared to that formulated using a standard matrix former, hydroxypropylmethylcellulose (HPMC). Hardness values ranged from 6.12 ± 1.80 to 9.73 ± 1.39 kgf, friability from 0.31 ± 0.00 to 1.00 ± 0.00%. The drug content ranged from 98 to 101 %. The percentage drug released from the matrix tablets after 10 h was between 71.27 and 98.73 % except for formulation BF3 that released 32.56 %. This study showed that sustained release diclofenac sodium matrix tablets were successfully formulated using Brachystegia eurycoma gum as the matrix former and the tablets were comparable to that formulated with HPMC. Keywords: Brachystegia eurycoma gum; Diclofenac sodium; Matrix tablets; Sustained release

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Li, Gui Yu, Xi Hong Lu, Xue Hu Li, Lei Tao, and Jian Ping Liang. "Preparation, Characterization and In Vitro Evaluation of IVM Loaded Poly(lactic-Co-Glycolic Acid) (PLGA) Microspheres." Advanced Materials Research 311-313 (August 2011): 1751–54. http://dx.doi.org/10.4028/www.scientific.net/amr.311-313.1751.

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Drug was encapsulated in a novel copolymers of poly(lactic-co-glycolic acid) (PLGA) to investigate the sustained-release formulation of drug loaded polymer microspheres delivery system. Used a modified solid-in-oil-in-water (S/O/W) emulsion solvent evaporation method to prepare microspheres, its morphology and particle size distribution were estimated by scanning electron microscopy (SEM), the profile of in vitro drug release were assessed by High performance liquid chromatography (HPLC). Finally, an stable release buffer was utilized to obtain a detailed drug release profile, which was analyzed by HPLC also. Results showed that the microspheres morphology, encapsulation efficiency and the cumulative drug release efficiency were appropriate for veterinary medicine using. The modified preparation method was simple and optimized, PLGA microspheres with excellent controlled-release characteristics may serve as drug delivery carrier and may prolong the drug sustained-release effect.

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Elder, Steven, John Graham Roberson, James Warren, Robert Lawson, Daniel Young, Sean Stokes, and Matthew K. Ross. "Evaluation of Electrospun PCL-PLGA for Sustained Delivery of Kartogenin." Molecules 27, no. 12 (June 10, 2022): 3739. http://dx.doi.org/10.3390/molecules27123739.

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In this study, kartogenin was incorporated into an electrospun blend of polycaprolactone and poly(lactic-co-glycolic acid) (1:1) to determine the feasibility of this system for sustained drug delivery. Kartogenin is a small-molecule drug that could enhance the outcome of microfracture, a cartilage restoration procedure, by selectively stimulating chondrogenic differentiation of endogenous bone marrow mesenchymal stem cells. Experimental results showed that kartogenin did not affect the electrospinnability of the polymer blend, and it had negligible effects on fiber morphology and scaffold mechanical properties. The loading efficiency of kartogenin into electrospun membranes was nearly 100%, and no evidence of chemical reaction between kartogenin and the polymers was detected by Fourier transform infrared spectroscopy. Analysis of the released drug using high-performance liquid chromatography–photodiode array detection indicated an abundance of kartogenin and only a small amount of its major hydrolysis product. Kartogenin displayed a typical biphasic release profile, with approximately 30% being released within 24 h followed by a much slower, constant rate of release up to 28 days. Although additional development is needed to tune the release kinetics and address issues common to electrospun scaffolds (e.g., high fiber density), the results of this study demonstrated that a scaffold electrospun from biodegradable synthetic polymers is a suitable kartogenin delivery vehicle.

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Sharafi, Mastaneh, Tyler White, Kelli Fowler, Kevin Ewell, Noe Galvan, and Nima Alamdari. "In Vitro Dissolution Evidence for Sustained and Prolonged Release of Vitamin C in a Phosphatidyl Choline-Enriched Lipid Encapsulation." Current Developments in Nutrition 5, Supplement_2 (June 2021): 1328. http://dx.doi.org/10.1093/cdn/nzab059_029.

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Abstract Objectives In vitro dissolution tests are valuable first-step tools in the development of bioavailable delivery systems, making it possible to assess the performance of novel technologies in releasing active ingredients through the amount dissolved in a dissolution medium. The objective of this study was to evaluate whether phosphatidyl choline-enriched lipid encapsulation releases the majority of vitamin C as ascorbic acid past the stomach in a standard in vitro dissolution procedure and to assess the release profile. Methods A novel phosphatidyl choline-enriched lipid encapsulation that is solid at room temperature was tested for dissolution in a standard dissolution apparatus according to compendial United States Pharmacopeia methods, as per Good Manufacturing Practices for dietary supplements. One serving (included 1000 mg ascorbic acid) was placed into vessels containing simulated gastric fluid (0.1 M HCl) for 120 minutes then changed to simulated intestinal fluid (buffered 2% sodium lauryl sulfate, pH 6.8) for an additional 360 minutes. Aliquots were tested for ascorbic acid concentration at 8 time points by titration. The data was compared with 1000 mg of regular ascorbic acid in a capsule format. Results The phosphatidyl choline-enriched lipid encapsulation released 36% of the vitamin C at 2 hours in the acid phase and released 56% at 3 hours, 67% at 4 hours, 85% at 6 hours and 98% at 8 hours in the intestinal phase. Regular vitamin C filled capsules released 100% of the vitamin C at 30 minutes. Conclusions The dissolution results indicated that phosphatidyl choline-enriched lipid encapsulation can pass the stomach and release the majority of vitamin C in the small intestine. The encapsulation demonstrated a sustained and prolonged release of vitamin C over an 8 hour period. The release profile observed in this in vitro study suggests phosphatidyl choline-enriched lipid encapsulation may improve nutrient absorption and bioavailability which requires further testing including human clinical trials. Funding Sources This study was supported by Lonza (Greenwood, SC) and Ritual (Natals Inc, Los Angeles, CA).

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Ryu, Suji, Seungyeop Park, Ha Yeon Lee, Hyungjun Lee, Cheong-Weon Cho, and Jong-Suep Baek. "Biodegradable Nanoparticles-Loaded PLGA Microcapsule for the Enhanced Encapsulation Efficiency and Controlled Release of Hydrophilic Drug." International Journal of Molecular Sciences 22, no. 6 (March 10, 2021): 2792. http://dx.doi.org/10.3390/ijms22062792.

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Recently, nano- and micro-particulate systems have been widely utilized to deliver pharmaceutical compounds to achieve enhanced therapeutic effects and reduced side effects. Poly (DL-lactide-co-glycolide) (PLGA), as one of the biodegradable polyesters, has been widely used to fabricate particulate systems because of advantages including controlled and sustained release, biodegradability, and biocompatibility. However, PLGA is known for low encapsulation efficiency (%) and insufficient controlled release of water-soluble drugs. It would result in fluctuation in the plasma levels and unexpected side effects of drugs. Therefore, the purpose of this work was to develop microcapsules loaded with alginate-coated chitosan that can increase the encapsulation efficiency of the hydrophilic drug while exhibiting a controlled and sustained release profile with reduced initial burst release. The encapsulation of nanoparticles in PLGA microcapsules was done by the emulsion solvent evaporation method. The encapsulation of nanoparticles in PLGA microcapsules was confirmed by scanning electron microscopy and confocal microscopy. The release profile of hydrophilic drugs can further be altered by the chitosan coating. The chitosan coating onto alginate exhibited a less initial burst release and sustained release of the hydrophilic drug. In addition, the encapsulation of alginate nanoparticles and alginate nanoparticles coated with chitosan in PLGA microcapsules was shown to enhance the encapsulation efficiency of a hydrophilic drug. Based on the results, this delivery system could be a promising platform for the high encapsulation efficiency and sustained release with reduced initial burst release of the hydrophilic drug.

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Rezk, Abdelrahman I., Jeesoo Park, Joon Yeon Moon, Sunny Lee, Chan Hee Park, and Cheol Sang Kim. "A Novel Design of Tri-Layer Membrane with Controlled Delivery of Paclitaxel and Anti-Biofilm Effect for Biliary Stent Applications." Nanomaterials 11, no. 2 (February 14, 2021): 486. http://dx.doi.org/10.3390/nano11020486.

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Here, we developed a novel biliary stent coating material that is composed of tri-layer membrane with dual function of sustained release of paclitaxel (PTX) anticancer drug and antibacterial effect. The advantages of using electrospinning technique were considered for the even distribution of PTX and controlled release profile from the nanofiber mat. Furthermore, film cast method was utilized to fabricate AgNPs-immobilized PU film to direct the release towards the tumor site and suppress the biofilm formation. The in vitro antibacterial test conducted against Gram-positive (Staphylococcus aureus) and Gram-negative (Escherichia coli) bacteria species showed excellent antibacterial effect. The in vitro drug release study confirmed the sustained release of PTX from the tri-layer membrane and the release profile fitted first order with correlation coefficient of R2 = 0.98. Furthermore, the release mechanism was studied using Korsmeyer–Peppas model, revealing that the release mechanism follows Fickian diffusion. Based on the results, this novel tri-layer membrane shows curative potential in clinical development.

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Wu, Yong Hui, Deng Guang Yu, Qian Su, Cheng Lei Cai, Ji An Zhang, and Jian Tao Zhang. "Electrosprayed PVP/Shellac Composite Medicated Microparticles for Providing Biphasic Drug Release Profile." Applied Mechanics and Materials 633-634 (September 2014): 562–66. http://dx.doi.org/10.4028/www.scientific.net/amm.633-634.562.

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The present study reports that a sustained release profile could be transferred into a biphasic drug release profile when a hydrophilic polymer was encapsulated into the medicated microparticles. The multiple component composite microparticles were fabricated using a single fluid electrospraying process to treat a co-dissolving solution consisting of a polymer matrix (shellac), an active ingredient (FA), and an additional hydrophilic polymer (poly vinyl pyrrolidone, PVP). FESEM results showed that the microparticles M1 consisting of shellac and FA had an average diameter of 1.27 ± 0.38 μm, whereas the microparticles M2 consisting of shellac, FA and PVP had an average diameter of 1.51 ± 0.34 μm. Both the two types of microparticles were essentially amorphous composites due to the favourable secondary interactions between the components, as demonstrated by ATR-FTIR tests. In vitro dissolution tests demonstrated that the addition of PVP in the microparticles M2 made them give a typical biphasic drug release profile, whereas the double-component microparticles provided a sustained release profile. This study shows a simple way for developing advanced drug delivery systems through tailoring the components of polymer excipients using electrospraying.

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Chongcherdsak, Noppadol, Direk Aekthammarat, Teerayuth Prathumchat, Chutima Limmatvapirat, and Sontaya Limmatvapirat. "Fabrication of Shellac-Zein Based Matrix Tablet as a Carrier for Controlling of Drug Release." Advanced Materials Research 1060 (December 2014): 50–53. http://dx.doi.org/10.4028/www.scientific.net/amr.1060.50.

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The aim of research was to fabricate shellac-zein composite polymer-based matrix tablets by using theophylline as a model drug. The tablets were prepared by direct compression process. The initial weight and hardness of tablets were controlled within the range of 300±5 mg and 60±10 N, respectively. The tablets were annealed at 80 °C for 24 h and kept in the ambient temperature before evaluation. Drug release profile and kinetics of drug release in 0.1 N HCl and buffer pH 6.8 were investigated. The result showed that the annealing process and shellac:zein ratio, affected drug release characteristic in both media.The delayed released in acid medium of formulation containg shellac-zein composite polymer at the ratio from 30:70 was extended to over 120 min. In addition, the more sustained drug released in buffer was observed after increasing shellac:zein ratio. The good acid resistance of shellac and the swollen characteristic of zein in buffer might be a good explanation for the specific release. For the analysis of drug release data, drug release profiles were fitted into Higuchi model suggesting that the main mechanism of drug release from matrix tablets was super case II transport.

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Wan, Dongwei, Min Zhao, Jingjing Zhang, and Libiao Luan. "Development and In Vitro-In Vivo Evaluation of a Novel Sustained-Release Loxoprofen Pellet with Double Coating Layer." Pharmaceutics 11, no. 6 (June 5, 2019): 260. http://dx.doi.org/10.3390/pharmaceutics11060260.

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This study aimed to develop a novel sustained release pellet of loxoprofen sodium (LXP) by coating a dissolution-rate controlling sub-layer containing hydroxypropyl methyl cellulose (HPMC) and citric acid, and a second diffusion-rate controlling layer containing aqueous dispersion of ethyl cellulose (ADEC) on the surface of a LXP conventional pellet, and to compare its performance in vivo with an immediate release tablet (Loxinon®). A three-level, three-factor Box-Behnken design and the response surface model (RSM) were used to investigate and optimize the effects of the citric acid content in the sub-layer, the sub-layer coating level, and the outer ADEC coating level on the in vitro release profiles of LXP sustained release pellets. The pharmacokinetic studies of the optimal sustained release pellets were performed in fasted beagle dogs using an immediate release tablet as a reference. The results illustrated that both the citric acid (CA) and ADEC as the dissolution- and diffusion-rate controlling materials significantly decreased the drug release rate. The optimal formulation showed a pH-independent drug release in media at pH above 4.5 and a slightly slow release in acid medium. The pharmacokinetic studies revealed that a more stable and prolonged plasma drug concentration profile of the optimal pellets was achieved, with a relative bioavaibility of 87.16% compared with the conventional tablets. This article provided a novel concept of two-step control of the release rate of LXP, which showed a sustained release both in vitro and in vivo.

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El-Kady, Abeer M., and Mohammad M. Farag. "Bioactive Glass Nanoparticles as a New Delivery System for Sustained 5-Fluorouracil Release: Characterization and Evaluation of Drug Release Mechanism." Journal of Nanomaterials 2015 (2015): 1–11. http://dx.doi.org/10.1155/2015/839207.

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Bioactive glass nanoparticles were synthesized and tested for the first time as a new delivery system for sustained 5-fluorouracil (5-FU) release. They were characterized by TEM, DTA, TGA, and FT-IR. The porosity % and specific surface area of glass nanoparticles were 85.59% and 378.36 m2/g, respectively. Thein vitrobioactivity evaluation confirmed that bioactive glass disks prepared from these nanoparticles could induce hydroxyapatite layer over their surfaces in simulated body fluid. Thein vitrodrug release experiment indicated that glass nanoparticles could serve as long-term local delivery vehicles for sustained 5-FU release. The release profile of 5-FU showed an initial fast release stage followed by a second stage of slower release. The initial burst release of 5-FU in the first day was about 23% (28.92 mg·L−1) of the total amount of loaded 5-FU, while the final cumulative percentage of the 5-FU released after 32 days was about 45.6% (57.31 mg·L−1) of the total amount of loaded 5-FU. The application of different mathematical models indicated that 5-FU was released by diffusion controlled mechanism and suggested that its release rate was dependent on glass particles dissolution, changes of surface area as well as diameter of glass particles, and concentration of loaded drug.

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De Luca, Mariana P., Juçara R. Franca, Filipe Augusto F. F. Macedo, Liliana Grenho, Maria Esperanza Cortes, André Augusto G. Faraco, Allyson N. Moreira, and Vagner R. Santos. "Propolis Varnish: Antimicrobial Properties against Cariogenic Bacteria, Cytotoxicity, and Sustained-Release Profile." BioMed Research International 2014 (2014): 1–6. http://dx.doi.org/10.1155/2014/348647.

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Varnishes are preparations that differ in the polymeric matrix and therapeutical agents. In dentistry they are used to prevent caries. In this study we developed a propolis varnish, considering propolis properties against cariogenic bacteria. To a chitosan polymeric base (CHV) was added ethanolic propolis extract in different concentrations: PV1 (5%), PV2 (10%), and PV3 (15%). Antimicrobial activity was carried out againstStreptococcus mutans(SM),Streptococcus sanguinis(SG),Streptococcus salivarius(SS), andLactobacillus casei(LC) through agar diffusion method. The three propolis concentrations incorporated were effective in inhibiting the growth of all microorganisms, but without significant difference between the zones of inhibition observed. Cytotoxicity assay was done by MTT method. Data were analyzed by one-way ANOVA and Bonferroni test. None of the varnishes were cytotoxic, keeping 80% of viable cells, while CHV allowed cellular proliferation (120%). Sustained-release test was carried out by applying 40 μL of each varnish in the buccal surface of bovine teeth and kept in an ethanol/water solution removed in regular times. According to the “independent model approach,” the release profiles were distinct from each varnish and the most prolonged was PV3 (8 weeks). Varnish formulations had satisfactory antimicrobial activity against cariogenic bacteria and have a low cytotoxicity (<50%).

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Kiew, Lik-Voon, Soon-Keng Cheong, Khalifah Sidik, and Lip-Yong Chung. "Improved plasma stability and sustained release profile of gemcitabine via polypeptide conjugation." International Journal of Pharmaceutics 391, no. 1-2 (May 2010): 212–20. http://dx.doi.org/10.1016/j.ijpharm.2010.03.010.

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Hai, Tao, Xi Wan, Deng-Guang Yu, Ke Wang, Yaoyao Yang, and Zhe-Peng Liu. "Electrospun lipid-coated medicated nanocomposites for an improved drug sustained-release profile." Materials & Design 162 (January 2019): 70–79. http://dx.doi.org/10.1016/j.matdes.2018.11.036.

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Akrami, Mohammad, Mehdi Khoobi, Masoud Khalilvand-Sedagheh, Ismaeil Haririan, Abbas Bahador, Mohammad Ali Faramarzi, Shahla Rezaei, et al. "Evaluation of multilayer coated magnetic nanoparticles as biocompatible curcumin delivery platforms for breast cancer treatment." RSC Advances 5, no. 107 (2015): 88096–107. http://dx.doi.org/10.1039/c5ra13838h.

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Y, Shravan Kumar, Shireesha G, and Harika S. "Formulation and Evaluation of Metoprolol Tartrate Sustained Release Matrix Tablets." International Journal of Pharmaceutical Sciences and Nanotechnology 12, no. 5 (September 30, 2019): 4865–671. http://dx.doi.org/10.37285/ijpsn.2019.12.5.7.

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The objective of the present work was to develop sustained release matrix tablets of Metoprolol tartrate using different polymers viz. Guar gum, Xanthan gum, Kondagogu gum and HPMC K100M. The release rates were modulated by combination of two different rates controlling material and triple mixture of two different rate controlling materials. After evaluation of physical properties of tablet, the in-vitro release study was performed in phosphate buffer pH 6.8 up to 12 hrs. Dissolution data was analyzed for release kinetics. It was observed that matrix tablets contained polymer Xanthan gum was successfully sustained the release of drug up to 12 hrs. Among all the formulations, F6 which contains 45 % of Xanthan gum, release of drug which follows zero order kinetics via, swelling, diffusion and the release profile of formulation F6 was compared with marketed product. The FTIR study revealed that there was no chemical interaction between drug and excipient.

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Singh, Jyoti Bhusan, Pramod Mourya, Gopal Rai, and Rajesh Shukla. "FORMULATION AND IN-VITRO EVALUATION OF NICARDIPINE HYDROCHLORIDE BILAYERED TABLET FOR CONTROLLED RELEASE." Journal of Advanced Scientific Research 13, no. 11 (December 31, 2022): 58–62. http://dx.doi.org/10.55218/jasr.2022131109.

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The aim of present research work was to prepare and evaluate the controlled release bilayered tablet of Nicardipine HCL to improve its bioavailability for the treatment of hypertension. To minimize critical process parameters, two layer compression method was used for the formulation of Bilayered tablets. The appropriate formulation was achieved successfully with the combination of Polymers MCC, Carbopol 71G and HPMC K100M produced desired release profile for Metoprolol succinate extended release layer. The combination of disintegrating agents that is Sodium starch glycolate and Dicalcium phosphate produced desired release rate for Nicardipine immediate release layer. The results reveal that formulation F7 has met the objective of controlled drug release for over a period of 12 hrs. The formulation F7 ascertained the efficacy of the controlled released Bilayered tablet of Nicardipine and Metoprolol ER tablet in hypertension. This sustained release Bilayered tablet with the combination of Nicardipine and metoprolol can be used in the management of different types of hypertension. The formulation F7 of combination of Nicardipine and metoprolol showed controlled release profile among the other, Hence it was considered as an optimized formulation.

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Hassanin, Ahmed, Ahmed A. El-Moneim, Mohamed Ghaniem, and Hassan Nageh. "Nanocomposite Multilayer Fibrous Membrane for Sustained Drug Release." Advanced Materials Research 894 (February 2014): 364–68. http://dx.doi.org/10.4028/www.scientific.net/amr.894.364.

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Building on the success of the many earlier studies on electrospun nanofibers technique which provide a non woven web to the order of nanometers introducing superior properties such as large surface area, superior mechanical properties and ease of implementation in many fields of applications, elctrospun nanofibers became an important issue for many researchers in various fields. Using elctrospun fibers as a drug carrier, is showing a huge promising potential for the future of biomedical application. Our work in this research is focusing on engineering a system to control the drug release profile rate especially for wound dressing. Nanocomposite multilayer fibrous membranes, using electrospinning method, have been developed for drug release in form of sandwich structure of three layers. Inner layer which is kept Polycaprolactane (PCL) loaded with drug. The two outer layers have been changed with different blend ratios between Chitosan (Cs) and PCL as follow [0%:100% Cs:PCL, 30%:70% Cs:PCL, 50%:50% Cs:PCL, 70%:30% Cs:PCL]. The results showed that the release rate has been affected dramatically by the outer layer composition. SEM images showed changing in the morphology due to the different in the composition of outer layer.

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Beg, Sarwar, Amit Kumar Nayak, Kanchan Kohli, Suryakanta Swain, and MS Hasnain. "Antimicrobial activity assessment of time-dependent release bilayer tablets of amoxicillin trihydrate." Brazilian Journal of Pharmaceutical Sciences 48, no. 2 (June 2012): 265–72. http://dx.doi.org/10.1590/s1984-82502012000200010.

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The aim of present study was the assessment of antimicrobial activity of prepared time-dependent release bilayer tablets of amoxicillin trihydrate and in vitro evaluation of drug release by antimicrobial assay using agar plate diffusion method. The bilayer tablets comprised of a delayed and sustained release layer. Direct compression method was used for the preparation of bilayer tablets containing Eudragit-L100 D55 as delayed release polymer, and HPMCK4M and HPMCK15 as sustained release polymers. The prepared bilayer tablets containing amoxicillin trihydrate were evaluated for hardness, thickness, friability, weight variation and drug content. Further, in vitro drug release was assessed by antimicrobial assay using S. aureus and E. coli as test microorganisms. The aliquot samples of in vitro drug release study were found to be effective against both microorganisms for 16 hours due to sustained action. The in vitro drug release study and antimicrobial assay showed that bilayer tablets have sustained release profile of drug delivery with time-dependent burst release after a lag-time of 2 hours. The lower MIC value (2 µg/mL) of prepared bilayer tablets vis-à-vis marketed preparation (5 µg/mL) represented its good antimicrobial activity.

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Journal articles on the topic 'Sustained release profile'

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