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Kuncahyo, Ilham, Shabrina Nindya Hutami, and RR Sri Wulandari. "PENGARUH TRANSCUTOL P DAN PEG 400 DALAM PEMBUATAN TABLET LIQUISOLID NIFEDIPIN TERHADAP MUTU FISIK DAN DISOLUSI." Cendekia Journal of Pharmacy 9, no. 1 (2025): 60–68. https://doi.org/10.31596/cjp.v9i1.330.
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Nifedipine as a hypertension drug has the problem of low solubility (BCS class II), leading to decreased dissolution and bioavailability. Formulation of nifedipine liquisolid using non-volatile solvents can overcome this problem. This study aimed to evaluate the effect of Transcutol P and PEG 400 as non-volatile liquisolid ingredients on the physical quality and dissolution of nifedipine liquisolid tablets. This study used seven nifedipine liquisolid formulations, each with varying concentrations of Transcutol P or PEG 400 as non-volatile solvents and lactose as carrier material. Formula 1 (20% Transcutol: 80% lactose), Formula 2 (25% Transcutol: 75% lactose), Formula 3 (30% Transcutol: 70% lactose), Formula 4 (20% PEG 400: 80% lactose), Formula 5 (25% PEG 400: 75% lactose), Formula 6 (30% PEG 400: 70% lactose), and one control formula. The nifedipine liquid produced from each formula was forged into tablets using the direct felting method with a weight of approximately 200 mg. The tablets were tested for physical quality and dissolution, and the results were statistically analyzed using SPSS version 12.0. The results showed that Transcutol P and PEG 400 as liquisolid ingredients for nifedipine tablets provided good physical quality and improved the quantity and rate of drug release. The effect of PEG 400 as a liquisolid material for nifedipine tablets slowed down the disintegration time and accelerated the dissolution rate compared with Transcutol P. The dissolution profile showed that the release of nifedipine tablets with PEG 400 liquisolid material reached 30% at the fifth minute, meeting the requirements according to Indonesian Pharmacopoeia VI, which stipulates that more than 75% should be released at the sixtieth minute
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Hashemzadeh, Nastaran, and Abolghasem Jouyban. "Review of Pharmaceutical Applications of Diethylene Glycol Monoethyl Ether." Journal of Pharmacy & Pharmaceutical Sciences 25 (November 6, 2022): 340–53. http://dx.doi.org/10.18433/jpps32921.
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Diethylene glycol monoethyl ether (DEGME) is a hydroalcoholic solvent that gained tremendous attention in the cosmetics, food, nanoformulations, and pharmaceutical industries. Due to its physicochemical features, it has been widely used as a penetration enhancer, surfactant, and solubilizer. Among numerous tradenames defined for DEGME -- Carbitol® (by Dow Chemical Co., USA), and Transcutol® HP, CG, and P. (by Gattefossé Co., France) -- are known to be employed in pharmaceutical industries. Transcutol® CG is utilized only in cosmetics; however, Transcutol® P and Carbitol® are both used in various pharmaceutical topical dosage forms such as creams, gels, etc. Additionally, Transcutol® HP is used in all administration routes. In view of this, the application of DEGME is highlighted in the areas of industry and pharmaceutical sciences. Moreover, in this review the prominent characteristics, pharmacokinetics, and toxicity of DEGME are examined and it is suggested that DEGME is a promising solvent/solubilizer with comparable assignments to other conventional excipients.
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Ojo, Olusola Emmanuel, Margaret Okonawan Ilomuanya, Ibilola Mary Cardoso-Daodu, et al. "Mupirocin/hydroxyapatite composite suspended in transcutol P-spiked hydrogel: In vitro characterization and in vivo wound healing assessment." American Journal of Pharmacotherapy and Pharmaceutical Sciences 3 (June 3, 2024): 11. http://dx.doi.org/10.25259/ajpps_2024_011.
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Objectives: Natural hydroxyapatite (HAP) has been utilized as a drug carrier owing to its excellent bioactivity and biocompatibility. This study is aimed at formulating mupirocin/hydroxyapatite composite suspended in hydrogel. The appropriate quantity of the penetration enhancer (Transcutol-P®) was also investigated. Materials and Methods: The HAP was isolated from bovine bone by hydrothermal treatment, calcined at 1000oC and held for 2 hours in an electric furnace to remove the organic contents. The bones were milled, sifted using 150 µm mesh sieve and characterized. Olive oil, which contains oleic acid, was utilized as a natural capping agent to prevent agglomeration of the particles in the formulation. The quantity of Transcutol-P® was varied with mupirocin used as the active pharmaceutical ingredient for the management of acute wound in Wistar rats. In this animal study, the wound closure rate was evaluated. Results: The formulation with the 0.6%v/v, of Transcutol-P® gave the best wound closure rate of 30.05 mm2/day. The in-vitro study showed that the formulation containing 0.6%v/v Transcutol-P® released 63.9% of the drug after 75 minutes while 42.4% was released at the same time interval when the concentration of the penetration enhancer was increased to 1.2%v/v. The mupirocin-encapsulated HAP hydrogel composite showed high resistance against staphylococcus saprophyticus with inhibition zone of 37.3 mm. Conclusion: The mupirocin encapsulated in HAP allows for sustained release of the antibiotic and thus serves as a veritable drug carrier suitable for wound healing applications. Transcutol-P® (0.6%v/v) is effective in facilitating drug release, which is reflected in the increased wound closure rate in Wistar rats.
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Date, Abhijit A., and Mangal S. Nagarsenker. "Single-step and low-energy method to prepare solid lipid nanoparticles and nanostructured lipid carriers using biocompatible solvents." European Journal of Pharmaceutical Research 1, no. 1 (2019): 12–19. http://dx.doi.org/10.34154/2019-ejpr.01(01).pp-12-19/euraass.
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Solid lipid nanoparticles (SLN) and nanostructured lipid carriers (NLCs) are widely being explored for improving dermal/transdermal and oral delivery of drugs, neutraceuticals and cosmeceuticals. High-pressure homogenization (HPH) is the most commonly used preparation method for SLN/NLCs. SLN/NLCs preparation by the HPH requires high energy input and longer duration. Here, we describe a simple yet innovative low-energy method to prepare SLN/NLCs in a single-step using biocompatible solvents. We first show that biocompatible solvents such as Transcutol P, Soluphor P, N-methyl pyrrolidone, and glycofurol can solubilize glyceryl monostearate, glyceryl behenate, and glyceryl distearate to a variable degree. Our pre-formulation studies showed that only GMS could be transformed into SLN or NLCs despite high solubility of the lipids investigated indicating the importance of solvent-lipid interaction parameter in our preparation method. Finally, we show that SLN and NLCs of glyceryl monostearate with size < 150 nm and acceptable polydispersity index can be easily developed using Transcutol P as a biocompatible solvent and polyoxyl-40-stearate (MYS-40) as a stabilizer. As the Transcutol P has excellent acceptability for dermal/transdermal and oral route, there is no need to remove the residual Transcutol P (5% v/v) from the prepared glyceryl monostearate SLN/NLCs. Thus, our method offers a simple yet innovative way to prepare GMS SLN/NLCs suitable for dermal/transdermal and oral applications.
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Pitzanti, Giulia, Antonella Rosa, Mariella Nieddu, et al. "Transcutol® P Containing SLNs for Improving 8-Methoxypsoralen Skin Delivery." Pharmaceutics 12, no. 10 (2020): 973. http://dx.doi.org/10.3390/pharmaceutics12100973.
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Topical psoralens plus ultraviolet A radiation (PUVA) therapy consists in the topical application of 8-methoxypsoralen (8-MOP) followed by the skin irradiation with ultraviolet A radiation. The employment of classical 8-MOP vehicles in topical PUVA therapy is associated with poor skin deposition and weak skin permeability of psoralens, thus requiring frequent drug administration. The aim of the present work was to formulate solid lipid nanoparticles (SLNs) able to increase the skin permeation of 8-MOP. For this purpose, the penetration enhancer Transcutol® P (TRC) was added to the SLN formulation. SLNs were characterized with respect to size, polydispersity index, zeta potential, entrapment efficiency, morphology, stability, and biocompatibility. Finally, 8-MOP skin diffusion and distribution within the skin layers was investigated using Franz cells and newborn pig skin. Freshly prepared nanoparticles showed spherical shape, mean diameters ranging between 120 and 133 nm, a fairly narrow size distribution, highly negative ζ potential values, and high entrapment efficiency. Empty and loaded formulations were almost stable over 30 days. In vitro penetration and permeation studies demonstrated a greater 8-MOP accumulation in each skin layer after SLN TRC 2% and TRC 4% application than that after SLN TRC 0% application. Finally, the results of experiments on 3T3 fibroblasts showed that the incorporation of TRC into SLNs could enhance the cellular uptake of nanoparticles, but it did not increase their cytotoxicity.
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Zainuddin, Siti Aisyah, Abdul Latip Ab Hamid, Aqila Iman Rafandi, Mashani Mohamad, Khuriah Abdul Hamid, and Syed Haroon Khalid. "The Effects of Different Solubilizing Agents on the Transport and Pharmacokinetic Profiles of Indocmethacin: In vitro and in vivo Approach." Sains Malaysiana 53, no. 11 (2024): 3747–59. http://dx.doi.org/10.17576/jsm-2024-5311-17.
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The poor water solubility of new chemical entities (NCEs) discovered in pharmaceutical screening programs hampers their development and limits effective treatment delivery. Solubilizing agents offer a direct approach to increase solubility and oral bioavailability. This study employed indomethacin as a model drug from Biopharmaceutical Classification System (BCS) class II. Solubilizing agents, including propylene glycol, Transcutol P, Labrasol, PEG 400, and Tween 80, were separately added at 10% (v/v) to 1 mg/5 mL for in vitro diffusion chamber and 10 mg/kg body weight for in vivo oral absorption studies of indomethacin. Drug concentrations were analysed using reversed-phase high-performance liquid chromatography (HPLC). In vitro, 10% (v/v) labrasol, PEG 400, and Tween 80 significantly (p<0.01) increased indomethacin permeability across the rat intestinal layer. However, Transcutol P and PG (propylene glycol 10%v/v) showed no discernible impact on in vitro permeability. In the in vivo oral absorption study, PG (propylene glycol 10%v/v) and Transcutol P significantly (p<0.05) enhanced indomethacin absorption, while 10% (v/v) labrasol, PEG 400, and Tween 80 did not show significant effects. No in vitro-in vivo correlation (IVIVC) was observed, likely due to the physicochemical properties of indomethacin and the complex physiological environment in the gastrointestinal (GI) tract. Further investigations are necessary to comprehensively understand the factors affecting indomethacin solubility and absorption, considering both the drug’s properties and the GI tract’s physiological conditions.
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Shin, Dong, Bo Chae, Yoon Goo, et al. "Improved Dissolution and Oral Bioavailability of Valsartan Using a Solidified Supersaturable Self-Microemulsifying Drug Delivery System Containing Gelucire® 44/14." Pharmaceutics 11, no. 2 (2019): 58. http://dx.doi.org/10.3390/pharmaceutics11020058.
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To improve the dissolution and oral bioavailability of valsartan (VST), we previously formulated a supersaturable self-microemulsifying drug delivery system (SuSMED) composed of Capmul® MCM (oil), Tween® 80 (surfactant), Transcutol® P (cosurfactant), and Poloxamer 407 (precipitation inhibitor) but encountered a stability problem (Transcutol® P-induced weight loss in storage) after solidification. In the present study, replacing Transcutol® P with Gelucire® 44/14 resulted in a novel SuSMED formulation, wherein the total amount of surfactant/cosurfactant was less than that of the previous formulation. Solidified SuSMED (S-SuSMED) granules were prepared by blending VST-containing SuSMED with selective solid carriers, L-HPC and Florite® PS-10, wherein VST existed in an amorphous state. S-SuSMED tablets fabricated by direct compression with additional excipients were sufficiently stable in terms of drug content and impurity changes after 6 months of storage at accelerated conditions (40 ± 2 °C and 75 ± 5% relative humidity). Consequently, enhanced dissolution was obtained (pH 1.2, 2 h): 6-fold for S-SuSMED granules against raw VST; 2.3-fold for S-SuSMED tablets against Diovan® (reference tablet). S-SuSMED tablets increased oral bioavailability in rats (10 mg/kg VST dose): approximately 177–198% versus raw VST and Diovan®. Therefore, VST-loaded S-SuSMED formulations might be good candidates for practical development in the pharmaceutical industry.
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Censi, Roberta, Valentina Martena, Ela Hoti, Ledjan Malaj, and Piera Di Martino. "Permeation and skin retention of quercetin from microemulsions containing Transcutol®P." Drug Development and Industrial Pharmacy 38, no. 9 (2011): 1128–33. http://dx.doi.org/10.3109/03639045.2011.641564.
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Yudanti, Gendis Purno, Ilham Kuncahyo, and Endang Diyah Ikasari. "Optimization of Naringenin Self-Nano Emulsifying Drug Delivery System (SNEDDS) Formula with D-optimal Mixture Design Method." Journal of Pharmaceutical Sciences and Community 21, no. 1 (2024): 100–108. http://dx.doi.org/10.24071/jpsc.004319.
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This study aimed to optimize and formulate the poorly water-soluble naringenin in the Self-Nano Emulsifying Drug Delivery System (SNEDDS) using D-optimal mixture design. D-optimal mixture design was used to optimize SNEDDS loading naringenin by selecting SNEDDS composition as an independent factor and SNEDDS characterization as a response. SNEDDS in the optimal formula were characterized, including transmittance, particle size, emulsification time, and drug loading. Triacetin, Tween 80, and transcutol p were respectively the selected oil, surfactant, and co-surfactant phases for their greatest ability to dissolve naringenin. The optimization results showed that the optimal formula was that using 10% triacetin, 70% of Tween 80, and 20% of transcutol p. SNEDDS loading naringenin produced nanoemulsion with 88.74±2.27 % of transmittance, 14.8 nm of particle size, 51.13 ± 4.53 mg/L of drug loading, and 18.58 ± 0.62 second of emulsification time. This study concludes that the D-optimal mixture design can be used to optimize and prepare the SNEDDS loading poorly-water soluble naringenin.
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Lee, Sang Gon, Jong Bu Kang, Sung Rae Kim, et al. "Enhanced topical delivery of tacrolimus by a carbomer hydrogel formulation with transcutol P." Drug Development and Industrial Pharmacy 42, no. 10 (2016): 1636–42. http://dx.doi.org/10.3109/03639045.2016.1160107.
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Yudanti, Gendis Purno, Ilham Kuncahyo, and Endang Diyah Ikasari. "In vitro Naringenin SNEDDS Release Test by Dissolution." Natural Sciences Engineering and Technology Journal 3, no. 2 (2022): 179–85. http://dx.doi.org/10.37275/nasetjournal.v3i2.29.
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Naringenin is the main flavanone in grapefruit which has anti-inflammatory, anti-cancer, hepatoprotective and antilipid peroxidation effects. Its low solubility in water causes dissolution and low bioavailability when taken orally. This study aims to increase the solubility and bioavailability of naringenin by using the SNEDDS technique. Initial characterization to determine the optimum formula was carried out using the D-optimal mixture design method, namely by optimizing the composition of SNEDDS which consisted of triacetin as the oil phase, tween 80 as surfactant and transcutol P as cosurfactant as an independent factor and SNEDDS characterization included emulsification time, drug loading, size globules and percent transmittance in response. The optimization results showed that the optimum formula was obtained at the composition of 10% triacetin, 70% tween 80 and 20% transcutol P. The dissolution test showed that the SNEDDS of naringenin was capable of dissolution (Q30) of 87,50% ±1,73 at the 30th minute and the f2 value of 28,93 so it can be concluded that the dissolution profile between the SNEDDS of naringenin and the naringenin capsules is not identical.
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Upadhye, Kanchan P., Divya Senpal, Minakshee Nimbalwar, and Gouri Dixit. "Formulation and Evaluation of Fish Oil-based Rizatriptan Microemulsion for Intranasal Migraine Treatment." International Journal of Pharmaceutical Sciences and Nanotechnology 8, no. 3 (2015): 2972–78. http://dx.doi.org/10.37285/ijpsn.2015.8.3.12.
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In the present study microemulsion based intranasal gel of rizatriptan using fish oil was prepared for treatment and management of migraine to sustain the drug release and improve the drug residence time in nasal cavity. Fish oil is reported to have antimigraine activity hence it has been used in the present formulation along with cremophore EL as surfactant and Transcutol P as co-surfactant. The pseudoternary phase diagram plotted with these components shown the microemulsion existence region in ratio of (1:9-9:1) surfactant and co-surfactant. The optimized micro-emulsion contained fish oil (45.29%), cremophore E/transcutol P (2:1) and was characterized for pH (6.3±0.02), viscosity (114 ± 3.00cp), % transmittance (99.5 ± 1.01), refractive index (1.335±0.01),). The prepared microemulsion gels were optimized and characterized for in-vitro studies, pH, drug content, rheological studies and stability study. The release of rizatriptan from micro-emulsion gel prepared from carbopol 934 (98.01%) was found to be higher and prolonged than plain gel. Thus, microemulsion based gel was able to prolong drug releaseand improve drug residence time in the nasal cavity.
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Chavda, Hitesh, Jaimeen Patel, Gordhan Chavada, Shruti Dave, Ankini Patel, and Chhagan Patel. "Self-Nanoemulsifying Powder of Isotretinoin: Preparation and Characterization." Journal of Powder Technology 2013 (November 13, 2013): 1–9. http://dx.doi.org/10.1155/2013/108569.
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In the present investigation an attempt was made to enhance the solubility and dissolution of poorly soluble drug, isotretinoin, by formulating self-nanoemulsifying drug delivery system (SNEDDS). Liquid SNEDDSs were prepared using Transcutol P as oil, Tween 80 as surfactant, and PEG 400 as cosurfactant. Pseudoternary phase diagrams were constructed to identify the efficient self-nanoemulsification region. The formulation with 40% oil (Transcutol P) and 60% surfactant: cosurfactant (Tween 80: PEG 400) ratio of 1 : 1 was optimized based on evaluation parameters for droplet size analysis, self-emulsification capacity, zeta potential, and in vitro drug release performance. The optimized system contains mean droplet size of 36.60 nm and zeta potential (ζ) −26.73 mV. The optimized formulation A1 was adsorbed onto Fujicalin to produce solid SNEDDS, which exhibited good flow properties and preserved the self-emulsification properties of liquid SNEDDS. The differential scanning calorimetry, FT-IR studies of solid SNEDDS revealed transformation of isotretinoin into molecularly dissolved state in the liquid SNEDDS. In vitro dissolution profiles showed that dissolution rate of ISN from solid SNEDDS was significantly greater as compared to pure drug.
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Virani, Amitkumar, Vinam Puri, Hana Mohd, and Bozena Michniak-Kohn. "Effect of Penetration Enhancers on Transdermal Delivery of Oxcarbazepine, an Antiepileptic Drug Using Microemulsions." Pharmaceutics 15, no. 1 (2023): 183. http://dx.doi.org/10.3390/pharmaceutics15010183.
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Oxcarbazepine (OXC) is an anticonvulsant drug, indicated for the treatment of the neurological disorder, epilepsy. The objective of the present study was to evaluate the transdermal delivery of OXC from microemulsions using different penetration enhancers. Transcutol® P (TRC), oleic acid (OA), cineole (cin), Labrasol (LS), Tween 80 (T80) and N-Methyl-Pyrrolidone (NMP) were used as penetration enhancers as well as microemulsion components. Simple formulations of OXC in propylene glycol (PG) incorporating various penetration enhancers and combination of penetration enhancers were also evaluated for transdermal delivery. Drug delivery and penetration enhancement were studied using human cadaver skin on Franz diffusion cells. The results showed that all penetration enhancers improved the rate of permeation of OXC compared to the control. The flux of drug delivery from the various formulations was found to be, in decreasing order, cin > OA + TRC > NMP > TRC > OA. Overall, microemulsions prepared using cineole, Tween 80 and Transcutol® P (TRC) were shown to be provide the best penetration enhancement for OXC.
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Mandal, Surjyanarayan, and Snigdha S. Mandal. "Microemulsion Drug Delivery System: A Platform for Improving Dissolution Rate of Poorly Water Soluble Drug." International Journal of Pharmaceutical Sciences and Nanotechnology 3, no. 4 (2011): 1214–19. http://dx.doi.org/10.37285/ijpsn.2010.3.4.6.
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The aim of the present study was to design novel o/w microemulsion of Glimepiride and to study its dissolution behavior by raising its solubility. Oil and surfactant were selected based on their drug solubilizing capacity and HLB value. Pseudoternary phase diagrams were developed at different ratios of Cremophor RH 40 and Transcutol P to know the microemulsion existing zone. Glimepiride loaded microemulsion using Labrafil M 1944 CS, Cremophor RH 40, Transcutol P as oil, surfactant and cosurfactant respectively, was prepared and characterized. Accelerated stability study of the developed microemulsion was carried out for 6 months. Drug solubilization capacity of the microemulsion system was determined. Solubility of Glimepiride by the O/W microemulsion was increased by 5785 times to that of water (0.019mg±0.002). In-vitro drug diffusion study revealed that after 10 hrs of diffusion, more than 18% of the drug was diffused from the microemulsion system, as compared to the commercially available tablets. Based on the results it could be concluded that microemulsion formulation could be used as a possible alternative to traditional oral formulations of Glimepiride to improve the dissolution rate and hence its bioavailability.
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Sanjay, Sahu, Jain Sachin, and Kumar Jain Neetesh. "Formulation, Development & Characterization of Self Nanoemulsifying Drug Delivery for Fenofibrate." Pharmaceutical and Chemical Journal 10, no. 3 (2023): 46–58. https://doi.org/10.5281/zenodo.13990679.
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The aim of the present investigation is to preparation, Development & Characterization of Self Nanoemulsifying Drug Delivery for Fenofibrate. Accurately weighed Fenofibrate was placed in a glass vial, and required quantity of oil, surfactant, and co-surfactant were added. The mixture was mixed by gentle stirring and vortex mixing at 40ºC on a magnetic stirrer at 200rpm, until Fenofibrate was dissolved. Capmul MCM was found satisfactory as oil, Cremophor RH 40 and Transcutol-P were found best as surfactant and cosurfactant on basis of solubility data. Selection of oil, surfactant and cosurfactant. The preliminary trials were carried out using different concentration of Capmul MCM oil, Cremophor RH 40 and Transcutol-P (3:1). On the basis of results of preliminary trials for selection of lipid vehicle, the concentration of Capmul MCM oil (X1) and Concentration of Cremophor RH 40: Transcutol-P (3:1) (X2) were taken as independent variables at three levels. In vitro drug release study was carried out for the formulations, Aliquots were collected periodically (10, 15, 20, 30, 45, 60 minutes) and replaced with fresh dissolution medium. Aliquots, after filtration through 0.45μ PVDF filter paper, were analyzed by HPLC at 248nm for Fenofibrate content. The study indicated that Cremophor RH 40 (HLB: 15) and Labrasol (HLB: 12) had very good ability to emulsify Capmul MCM oil followed by Tween 80 (HLB: 15), whereas, Cremophor EL (HLB: 13) and Labrafac PG (HLB: 1) appeared to be poor emulsifier for Capmul MCM oil. Fenofibrate and Excipients were mixed in 1:1 ratio. It was analysed at 40ºC/75% RH at Initial and 1 month by IR Spectroscopy. The 32 factorial design was employed using concentration of Capmul MCM oil and concentration of surfactant/Cosurfactant as independent variable X1 and X2 respectively. The Globule size (GS) (Y1), Polydispersity index (PDI) (Y2), Zeta potential (Y3), drug release at 15 minutes of Fenofibrate (Y4). SNEDDS is best suited for dosage for development of poorly soluble drugs. Fenofibrate are BCS class II drugs having low solubility and high permeability.
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Sisinthy, Sreenivas Patro, Nalamolu Koteswara Rao, and Chin Yi Lynn Sarah. "DESIGN, OPTIMIZATION AND IN VITRO CHARACTERIZATION OF SELF NANO EMULSIFYING DRUG DELIVERY SYSTEM OF OLMESARTAN MEDOXOMIL." International Journal of Pharmacy and Pharmaceutical Sciences 9, no. 1 (2016): 94. http://dx.doi.org/10.22159/ijpps.2017v9i1.15166.
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<p><strong>Objective: </strong>The objective of the present study was to design, optimise and characterise self nano emulsifying drug delivery systems (SNEDDS) for a poorly water soluble drug, olmesartan medoxomil (OLM) by Formulation by Design (FbD) approach with an aim to improve its solubility and dissolution.</p><p><strong>Methods: </strong>The SNEDDS were systematically optimised using three factor Box-Behnken design. Concentration of formulation variables, namely, the oil phaseX1 (Capryol 90), the surfactant X2 (Cremophor EL), and the co-surfactant X3 (Transcutol P), was optimized for its impact on mean globule size (Y1), percentage drug release in 20 min (Y2) and turbidity (Y3) of the formulation. Ternary phase diagrams were constructed to select the areas of nanoemulsion and the amounts of oil, surfactant and cosurfactants as critical formulation variables. The prepared SNEDDS were characterised for globule size, dissolution studies, turbidity, and transmission electron microscopy (TEM).</p><p><strong>Results: </strong>Following optimisation, the values of formulation variables were found to be 142.276 mg (Capryol P), 399.999 mg (Cremophor EL) and 598.871 mg (Transcutol P) which produced a globule size of 12.64 nm, percentage drug release of 93.34% and a turbidity of 0.02 FNU. TEM studies demonstrated spherical droplet morphology.</p><p><strong>Conclusion: </strong>Thus, the present studies reveal that the SNEDDS is a promising drug delivery system approach for the enhancement of solubility and dissolution rate of OLM.</p>
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Solanki, Shailendra Singh, Brajesh Sarkar, and Rakesh Kumar Dhanwani. "Microemulsion Drug Delivery System: For Bioavailability Enhancement of Ampelopsin." ISRN Pharmaceutics 2012 (July 8, 2012): 1–4. http://dx.doi.org/10.5402/2012/108164.
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Ampelopsin, one of the most common flavonoids, reported to possess numerous pharmacological activities and shows poor aqueous solubility. The purpose of this study was to enhance the dissolution rate and bioavailability of this drug by developing a novel delivery system that is microemulsion (ME) and to study the effect of microemulsion (ME) on the oral bioavailability of ampelopsin. Capmul MCM-based ME formulation with Cremophor EL as surfactant and Transcutol as cosurfactant was developed for oral delivery of ampelopsin. Optimised ME was evaluated for its transparency, viscosity, percentage assay and so forth. Solubilisation capacity of the ME system was also determined. The prepared ME was compared with the pure drug solution and commercially available tablet for in vitro drug release. The optimised ME formulation containing ampelopsin, Capmul MCM (5.5%), Cremophor EL (25%), Transcutol P (8.5%), and distilled water showed higher in vitro drug release, as compared to plain drug suspension and the suspension of commercially available tablet. These results demonstrate the potential use of ME for improving the bioavailability of poor water soluble compounds, such as ampelopsin.
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Neelam Brinda Gouri, M Sunitha Reddy, and K. Anie Vijetha. "Formulation and evaluation of posaconazole Emulgel: A novel topical drug delivery." GSC Biological and Pharmaceutical Sciences 29, no. 3 (2024): 045–61. https://doi.org/10.30574/gscbps.2024.29.3.0442.
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The goal of this study is to create a Posaconazole emu gel that will enable the medication to permeate the skin more deeply than current preparations. Posaconazole, a triazole antifungal medication, is used to prevent severe fungal infections. When administered orally, this medication absorbs slowly. Topical pharmaceutical delivery is preferred as a therapy method because it prevents the drug's first-pass metabolism. Posaconazole emu gel is prepared using the gelling agent carbopol 934. Furthermore, oleic acid is used as an emulsifier for the oil phase, while tween 80 is used as an emulsifier for the aqueous phase, propylene glycol and Transcutol P serves as a co-surfactant and Transcutol in this formulation has used for its ability to enhance anti- fungal property, and methyl paraben and propyl paraben are employed as preservatives. TEA (Triethanolamine) was Added to adjust the pH of the emu gel to 6-6.5. All of the prepared emulgels had satisfactory physical properties. The batch F6 of the formulation demonstrates improved drug release compared to the other formulations
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Neelam, Brinda Gouri, Sunitha Reddy M, and Anie Vijetha K. "Formulation and evaluation of posaconazole Emulgel: A novel topical drug delivery." GSC Biological and Pharmaceutical Sciences 29, no. 3 (2024): 045–61. https://doi.org/10.5281/zenodo.14829663.
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The goal of this study is to create a Posaconazole emu gel that will enable the medication to permeate the skin more deeply than current preparations. Posaconazole, a triazole antifungal medication, is used to prevent severe fungal infections. When administered orally, this medication absorbs slowly. Topical pharmaceutical delivery is preferred as a therapy method because it prevents the drug's first-pass metabolism. Posaconazole emu gel is prepared using the gelling agent carbopol 934. Furthermore, oleic acid is used as an emulsifier for the oil phase, while tween 80 is used as an emulsifier for the aqueous phase, propylene glycol and Transcutol P serves as a co-surfactant and Transcutol in this formulation has used for its ability to enhance anti- fungal property, and methyl paraben and propyl paraben are employed as preservatives. TEA (Triethanolamine) was Added to adjust the pH of the emu gel to 6-6.5. All of the prepared emulgels had satisfactory physical properties. The batch F6 of the formulation demonstrates improved drug release compared to the other formulations
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Darna, Bhikshapathi, and Bommareddy Srinivasa Padma Ganesh. "Development and In vivo Evaluation of Pitavastatin Self-emulsifying Drug Delivery Systems." International Journal of Pharmaceutical Sciences and Drug Research 13, no. 03 (2020): 295–302. http://dx.doi.org/10.25004/ijpsdr.2021.130309.
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The current research was intended at formulation and in vivo evaluation of pitavastatin self-nano emulsifying drug delivery system (PTN SNEDDS) for enhanced drug dissolution and bioavailability. Solubility studies carried out to construct pseudoternary phase diagram employing the blends of oil (capmulPG8), surfactant (acrysol K140), and cosurfactant (transcutol P). The PNT SNEDDS was prepared and optimized by adopting response surface methodology employing a 33 Box-Behnken design. The SNEDDS formulations characterized for % drug content, % entrapment efficiency, in-vitro release studies, particle size, zeta potential, Fourier Transform Infrared Spectroscopy (FTIR), and scanning electron microscopy (SEM) studies. The bioavailability studies were carried out in Wistar rats. The study indicated that PTN12 comprising of 40% capmul PG8, 40% acrysol K140, and 30% transcutol P displayed minimum droplet size (24.8nm), optimal zeta potential (-10.4 mV), and maximum drug release (98.75%). The SEM data revealed that droplet size is in the nanometer range. The pharmacokinetic studies conducted in rats indicated that Cmax of optimized PTN SNEDDS (2.25±0.02ng/mL) was higher than pure PTN suspension (0.75±0.03ng/mL) and optimized SNEDDS exhibited superior oral bioavailability about 4 times of AUC, along with higher plasma concentration than pure drug. The above results indicated that the application of SNEDDS formulation technique for PTN increases solubility and dissolution
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Prajapati, Shailesh T., Harsh A. Joshi, and Chhaganbhai N. Patel. "Preparation and Characterization of Self-Microemulsifying Drug Delivery System of Olmesartan Medoxomil for Bioavailability Improvement." Journal of Pharmaceutics 2013 (September 24, 2013): 1–9. http://dx.doi.org/10.1155/2013/728425.
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Olmesartan medoxomil (OLM) is an angiotensin II receptor blocker (ARB) antihypertensive agent administered orally that has absolute bioavailability of only 26% due to the poor aqueous solubility (7.75 μg/ml). The aim of the present investigation was to develop a self-microemulsifying drug delivery system (SMEDDS) to enhance the oral absorption of OLM. The solubility of OLM in various oils, surfactants, and cosurfactants was determined. Pseudoternary phase diagrams were constructed using Acrysol EL 135, Tween 80, Transcutol P, and distilled water to identify the efficient self-microemulsification region. Prepared SMEDDS was further evaluated for its emulsification time, drug content, optical clarity, droplet size, zeta potential, in vitro dissolution, and in vitro and ex vivo drug diffusion study. The optimized formulation S2 contained OLM (20 mg), Tween 80 (33%v/v), Transcutol P (33%v/v), and Acrysol EL 135 (34%v/v) had shown the smallest particle size, maximum solubility, less emulsification time, good optical clarity, and in vitro release. The in vitro and ex vivo diffusion rate of the drug from the SMEDDS was significantly higher than that of the plain drug suspension. It was concluded that SMEDDS would be a promising drug delivery system for poorly water-soluble drugs by the oral route.
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Sanjay, Sahu, Kumar Jain Sachin, and Kumar Jain Neetesh. "Formulation, Development & Characterization of Self Nanoemulsifying Drug Delivery for Fenofibrate." Journal of Scientific and Engineering Research 10, no. 6 (2023): 26–38. https://doi.org/10.5281/zenodo.10462487.
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<strong>Abstract </strong>The aim of the present investigation is to preparation, Development & Characterization of Self Nanoemulsifying Drug Delivery for Fenofibrate. Accurately weighed Fenofibrate was placed in a glass vial, and required quantity of oil, surfactant, and co-surfactant were added. The mixture was mixed by gentle stirring and vortex mixing at 40ºC on a magnetic stirrer at 200rpm, until Fenofibrate was dissolved. Capmul MCM was found satisfactory as oil, Cremophor RH 40 and Transcutol-P were found best as surfactant and cosurfactant on basis of solubility data. Selection of oil, surfactant and cosurfactant. The preliminary trials were carried out using different concentration of Capmul MCM oil, Cremophor RH 40 and Transcutol-P (3:1). On the basis of results of preliminary trials for selection of lipid vehicle, the concentration of Capmul MCM oil (X1) and Concentration of Cremophor RH 40: Transcutol-P (3:1) (X2) were taken as independent variables at three levels. In vitro drug release study was carried out for the formulations, Aliquots were collected periodically (10, 15, 20, 30, 45, 60 minutes) and replaced with fresh dissolution medium. Aliquots, after filtration through 0.45μ PVDF filter paper, were analyzed by HPLC at 248nm for Fenofibrate content. The study indicated that Cremophor RH 40 (HLB: 15) and Labrasol (HLB: 12) had very good ability to emulsify Capmul MCM oil followed by Tween 80 (HLB: 15), whereas, Cremophor EL (HLB: 13) and Labrafac PG (HLB: 1) appeared to be poor emulsifier for Capmul MCM oil. Fenofibrate and Excipients were mixed in 1:1 ratio. It was analysed at 40ºC/75% RH at Initial and 1 month by IR Spectroscopy. The 3<sup>2</sup> factorial design was employed using concentration of Capmul MCM oil and concentration of surfactant/Cosurfactant as independent variable X1 and X2 respectively. The Globule size (GS) (Y1), Polydispersity index (PDI) (Y2), Zeta potential (Y3), drug release at 15 minutes of Fenofibrate (Y4). SNEDDS is best suited for dosage for development of poorly soluble drugs. Fenofibrate are BCS class II drugs having low solubility and high permeability.
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Kazi, Mohsin, Ahmad A. Shahba, Saad Alrashoud, Majed Alwadei, Abdelrahman Y. Sherif, and Fars K. Alanazi. "Bioactive Self-Nanoemulsifying Drug Delivery Systems (Bio-SNEDDS) for Combined Oral Delivery of Curcumin and Piperine." Molecules 25, no. 7 (2020): 1703. http://dx.doi.org/10.3390/molecules25071703.
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Background: Bioactive oils of natural origin have gained huge interests from health care professionals and patients. Objective: To design a bioactive self-nanoemulsifying drug delivery system (Bio-SNEDDS) comprising curcumin (CUR) and piperine (PP) by incorporating bioactive natural oils in the formulation. Methods: The self-emulsifying properties of apricot, avocado, black seed and Zanthoxylum rhetsa seed oils were screened within various SNEDDS formulations. Each liquid SNEDDS formulation was loaded with both CUR and PP. The optimal liquid SNEDDS were solidified using Aeroperl® and Neusilin® at 1:1 w/w ratio. Liquid and solid SNEDDS were characterized by droplet size analysis, equilibrium solubility, scanning electron microscopy, X-ray powder diffraction, differential scanning calorimetry, and Fourier transform infrared spectroscopy. In-vitro dissolution studies were performed to evaluate the efficiency of CUR and PP release from solid Bio-SNEDDS. Results: The liquid SNEDDS comprised of black seed oil exhibited excellent self-emulsification performance, low droplet size along with transparent appearance. The inclusion of the cosolvent Transcutol P improved the solubilization capacity of both CUR and PP. The liquid SNEDDS were efficiently solidified using the two adsorbents and presented the drugs within amorphous state. In particular, SNEDDS comprised of black seed oil/Imwitor988/Transcutol P/Cremophor RH40 (20/20/10/50) and when solidified with Neusilin showed enhanced CUR and PP release (up to 60% and 77%, respectively). In addition, this formulation efficiently delivers the highly bioactive black seed oil to the patient. Conclusions: The optimized Bio-SNEDDS comprising black seed oil showed outstanding self-emulsification characteristics along with enhanced CUR/PP dissolution upon solidification.
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Ricardo, I. Komang Aan Adi, and Dewa Ayu Arimurni. "Optimization of self-nano emulsifying drug delivery system of rifampicin for nebulization using cinnamon oil as oil phase." Pharmaciana 14, no. 3 (2024): 356–69. https://doi.org/10.12928/pharmaciana.v14i3.28892.
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Lung delivery can overcome the problems related to the effectiveness of tuberculosis treatment by increasing the drug concentration at the target site. Rifampicin as the first-line antibiotic for tuberculosis has low water solubility and is unstable in gastric which hinders its effectiveness. Self-nanoemulsifying drug delivery system (SNEDDS) is a strategy known to improve the solubility and stability of such drugs. This study aimed to obtain the optimum formula of rifampicin SNEDDS intended for lung nebulization using essential oil as an oil phase. Several essential oils are known to have effective antibacterial on Mycobacterium tuberculosis. However, a high capability to solubilize the drug is required for SNEDDS formulation. Cinnamon oil, tween 80, and transcutol P were chosen as SNEDDS components for optimization using a D-optimal mixture based on the physicochemical characteristics. The optimum formula comprised 12.65% cinnamon oil, 75.00% tween 80, and 12.35% transcutol P which dispersed easily to form a highly transparent emulsion in normal saline under 1 minute. Upon dilution with saline, the optimal SNEDDS can produce a homogenous nanometer droplet (169.2±19.771 nm, PDI of 0.258±0.070) with acceptable pH for lung administration. It also has a viscosity similar to water (0.94±0.01 cP) which allows it to be nebulized easily (aerosol output rate of 0.14±0.02 g/min). Although the diluted SNEDDS has a zeta potential of -2.533±0.268 mV, it was stable for up to 4 hours during the nebulization. These results indicate the potential of cinnamon oil-based rifampicin SNEDDS to be an alternative in the pulmonary delivery of rifampicin via nebulization.
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Lee, Su Man, Ju Hwan Jeong, Jeong Gyun Lee, and Kyeong Soo Kim. "Development of Nilotinib HCl-loaded solid SNEDDS (Self-Nanoemulsifying Drug Delivery System) using Mesoporous Colloidal Silica." Yakhak Hoeji 67, no. 6 (2023): 378–87. http://dx.doi.org/10.17480/psk.2023.67.6.378.
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The objective of this study was to develop a novel nilotinib HCl-loaded solidified self-nanoemulsifying drug delivery system (SNEDDS) formulation with enhanced solubility and dissolution rate. Various oils and surfactants were screened, resulting in the selection of Peceol (oil) and Tween 80 (surfactant) and Transcutol P (co-surfactant). Pseudoternary phase diagram was constructed to detect the nanoemulsion zone. Among the SNEDDS formulations tested, the SNEDDS consisting of Peceol (oil), Tween 80 (surfactant), and Transcutol P (co-surfactant) at a weight ratio of 30/50/20 produced an emulsion droplet size of 182.1±1.0 nm. The spray drying technique, using mesoporous silicon dioxide as an inert carrier, was employed to solidify the selected nilotinib HCl-loaded SNEDDS. The resulting nilotinib HCl-loaded solid SNEDDS (S-SNEDDS) was characterized by scanning electron microscopy (SEM), powder X-ray diffractometry (PXRD), dynamic light scattering, saturation solubility and in vitro dissolution study. The S-SNEDDS produced an emulsion droplet size of 185.2±0.9 nm and there was no change in emulsion particle size upon the addition of drug. SEM and PXRD results suggested that nilotinib HCl existed in an amorphous form in nilotinib HCl-loaded S-SNEDDS. Solubility tests across various pH levels showed a significant improvement in nilotinib HCl solubility. Similarly, dissolution tests demonstrated enhanced dissolution rates in all tested solutions, consistent with the solubility results. These results indicate that the employed methodologies were effective in increasing both the solubility and dissolution rates of nilotinib HCl across different pH environments, suggesting a successful enhancement of its bioavailability.
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Shakeel, Faiyaz, Mohd Imran, Nazrul Haq, Sultan Alshehri, and Md Khalid Anwer. "Synthesis, Characterization and Solubility Determination of 6-Phenyl-pyridazin-3(2H)-one in Different Pharmaceutical Solvents." Molecules 24, no. 18 (2019): 3404. http://dx.doi.org/10.3390/molecules24183404.
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The current research work proposed the solubility data and solution thermodynamic properties of the cardiovascular agent 6-phenylpyridazin-3(2H)-one [PPD] in twelve pharmaceutical solvents at “T = 298.2 K to 318.2 K” and “p = 0.1 MPa”. The measured solubilities of PPD were regressed well with “van’t Hoff and Apelblat models”. The solid phases of pure and equilibrated PPD were characterized using differential scanning calorimetry and powder X-ray differactometry, and the results suggested no transformation of PPD into solvates/hydrates/polymorphs after equilibrium. The solubilities of PPD in a mole fraction at “T = 318.2 K” were noted at a maximum in dimethyl sulfoxide (DMSO, 4.73 × 10−1), followed by polyethylene glycol-400 (PEG-400, 4.12 × 10−1), Transcutol® (3.46 × 10−1), ethyl acetate (EA, 81 × 10−2), 2-butanol (2.18 × 10−2), 1-butanol (2.11 × 10−2), propylene glycol (PG, 1.50 × 10−2), isopropyl alcohol (IPA, 1.44 × 10−2), ethylene glycol (EG, 1.27 × 10−2), ethanol (8.22 × 10−3), methanol (5.18 × 10−3) and water (1.26 × 10−5). Similar tendencies were also noted at other studied temperatures. The results of the “apparent thermodynamic analysis” showed an endothermic and entropy-driven dissolution of PPD in all pharmaceutical solvents. The results of the activity coefficients suggested a maximum interaction at the molecular level in PPD-DMSO, PPD-PEG-400 and PPD-Transcutol, compared with other combination of the solute and solvents.
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Kumar, Bimlesh, Varun Garg, Amarjeet Singh, et al. "INVESTIGATION AND OPTIMIZATION OF FORMULATION PARAMETERS FOR SELFNANOEMULSIFYING DELIVERY SYSTEM OF TWO LIPOPHILIC AND GASTROINTESTINAL LABILE DRUGS USING BOX-BEHNKEN DESIGN." Asian Journal of Pharmaceutical and Clinical Research 11, no. 14 (2018): 12. http://dx.doi.org/10.22159/ajpcr.2018.v11s2.28585.
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Objective: Present research work aims toward codelivery of two hydrophobic drugs, curcumin (CRM) and duloxetine hydrochloride (DXH) through self-nanoemulsifying drug delivery systems (SNEDDS).Methods: Initially, binary mixture in the ratio of 1:1 was prepared and then loaded into SNEDDS. Box-Behnken design (BBD) was adopted to develop SNEDDS. As per the optimal design, 13 SNEDDS prototypes were prepared. Castor oil, tween-80 and Transcutol P® were used as oil, surfactant, and cosurfactant, respectively. To 1 mL of SNEDDS, 30 mg each of CRM and DXH was loaded (CRM-DXH- SNEDDS).Results: The design revealed that for mean droplet size, polydispersity index (PDI), as well as percentage drug loading, all the three factors, i.e. ratio of oil (a), surfactant (b), and cosurfactant (c) were found to give significant effect. Factor B showed the most significant effect on mean droplet size (y1). In case of PDI (y2), factors B and C exerted maximum influence, whereas, Factor A has shown non-significant effect. For percentage drug loading of drugs (y3 and y4), all the three factors were found to have the most significant effect. The optimized batch of CRM-DXH- SNEDDS having composition castor oil, tween-80, and Transcutol P® in the ratio: 2.17:5.22:2.61, revealed that the mean drug loading (%) of CRM and DXH in an optimized batch of SNEDDS was found to be 87.22±1.87 and 92.32±0.19%, respectively. The mean droplet size, PDI, and zeta potential of formed SNEDDS were observed as 113.14±1.14 nm, 0.20±0.026, and −13.2 mV, respectively.Conclusion: BBD provided optimal formula composition for SNEDDS for obtaining desirable drug loading, emulsion droplet size, and zeta potential.
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Lee, Jong-Hwa, and Gye-Won Lee. "Formulation Approaches for Improving the Dissolution Behavior and Bioavailability of Tolvaptan Using SMEDDS." Pharmaceutics 14, no. 2 (2022): 415. http://dx.doi.org/10.3390/pharmaceutics14020415.
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Tolvaptan, a selective vasopressin receptor antagonist, is a Class IV agent of Biopharmaceutical Classification System (BCS). To improve bioavailability after oral administration, the new tolvaptan-loaded self-microemulsifying drug delivery system (SMEDDS) was further optimized using a “design of the experiment (DoE)” including components of D-optional mixture design. Based on a solubility study of tolvaptan in various oils, surfactants, and cosurfactants, Capryol® 90, Tween 20, and Transcutol® HP [or polyethylene glycol 200 (PEG 200)] were finally selected for optimization of tolvaptan-loaded SMEDDS formulations. The fitting models of, and poly-nominal equations for, all response variables were acceptable, as revealed by analysis of variance (ANOVA, R2 > 0.900, p < 0.0001). The optimized formulations A-1 (Capryol® 90/Tween 20/Transcutol® HP = 10%/70%/20% w/w) and B-1 (Capryol® 90/Tween 20/PEG 200 = 10%/70%/20% w/w) with desirabilities of 0.905 and 1.000, respectively, showed low droplet size and the dissolution rate exceeded 95% at 15 and 60 min. The tolvaptan-loaded SMEDDS remained stable for 3 months under accelerated conditions, thus with no change in any of content, color, particle size, or dissolution rate. In a rat pharmacokinetic study, the bioavailability of formulations A-1 (16.6%) and B-1 (11.5%) were 23–33-fold higher than that of raw tolvaptan powder (0.5%). Thus, the use of “quality by design (QbD)” during development of tolvaptan-loaded SMEDDS improved the dissolution rate and oral drug bioavailability.
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Hammodi, Ihab D., and Shaimaa N. Abd Alhammid. "Preparation and Characterization of Topical Letrozole Nanoemulsion for Breast Cancer." Iraqi Journal of Pharmaceutical Sciences ( P-ISSN: 1683 - 3597 , E-ISSN : 2521 - 3512) 29, no. 1 (2020): 195–206. http://dx.doi.org/10.31351/vol29iss1pp195-206.
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Letrozole (LZL) is a non-steroidal competitive aromatase enzyme system inhibitor. The aim of this study is to improve the permeation of LZL through the skin by preparing as nanoemulsion using various numbers of oils, surfactants and co-surfactant with deionized water. Based on solubility studies, mixtures of oleic acid oil and tween 80/ transcutol p as surfactant/co-surfactant (Smix) in different percentages were used to prepare nanoemulsions (NS). Therefore, 9 formulae of (o/w) LZL NS were formulated, then pseudo-ternary phase diagram was used as a useful tool to evaluate the NS domain at Smix ratios: 1:1, 2:1 and 3:1.
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Janapareddi, Krishnaveni, and Anilgoud Kandhula. "Development and Ex vivo evaluation of Rasagiline Mesylate mucoadhesive microemulsion for intranasal delivery using Box-Behnken design." International Journal of Bio-Pharma Research 8, no. 3 (2019): 2514–22. http://dx.doi.org/10.21746/aps.2018.8.3.4.
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Rasagiline mesylate (RM), an irreversible, selective inhibitor of MAO-B enzyme, is used in the treatment of Parkinson’s disease as oral tablets. It has low oral bioavailability (36%) due to hepatic first pass metabolism. Oral route of administration is associated with nausea and vomiting. Hence present research work was aimed to develop intranasal RM- loaded mucoadhesive microemulsions for brain targeting via olfactory pathway. The microemulsions were developed using Box Behnken design and evaluated for globule size, PDI, Zeta potential, pH, viscosity and ex vivo permeation on excised porcine nasal mucosa. Based on drug solubility, Capmul MCM, Tween 20 and Transcutol P were selected as oil, surfactant and cosurfactant respectively. Microemulsions were prepared by water titration method. Pseudoternary phase diagrams were constructed and the levels of surfactants, oil were selected. The influence of independent variables such as oil, Smix and water on responses size, zeta potential and flux were studied with the help of polynomial equations, contour plots and 3D response surface plots generated by design expert software. Optimized microemulsion formulation (ME18) was composed of oil (Capmul MCM), Smix (Tween 20: Transcutol P; 1:1), water and drug in the ratio 5:42:65:5.The globule size, zeta potential and flux of the optimized microemulsion was 150 nm, -29.6 mV and 291.7 μg/cm2/h respectively. Mucoadhesive agent (Chitosan) was added at 0.5% concentration to optimized microemulsion formulation (MME18). The size, zeta potential and flux of the MME18 was 176.4 nm, 12.1 mV and 323.1 μg/cm2/h respectively. The flux of ME18 and MME 18 was significantly higher than drug solution. The enhancement ratio of MME 18 was 4.2 times to that of drug solution, indicating potential advantage of microemulsion formulation.
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Morakul, Boontida, Varaporn Buraphacheep Junyaprasert, Krisada Sakchaisri, and Veerawat Teeranachaideekul. "Cannabidiol-Loaded Nanostructured Lipid Carriers (NLCs) for Dermal Delivery: Enhancement of Photostability, Cell Viability, and Anti-Inflammatory Activity." Pharmaceutics 15, no. 2 (2023): 537. http://dx.doi.org/10.3390/pharmaceutics15020537.
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The aim of this study was to encapsulate cannabidiol (CBD) extract in nanostructured lipid carriers (NLCs) to improve the chemical stability and anti-inflammatory activity of CBD for dermal delivery. CBD-loaded NLCs (CBD-NLCs) were prepared using cetyl palmitate (CP) as a solid lipid and stabilized with Tego® Care 450 (TG450) or poloxamer 188 (P188) by high-pressure homogenization (HPH). The CBD extract was loaded at 1% w/w. Three different oils were employed to produce CBD-NLCs, including Transcutol® P, medium-chain triglycerides (MCT), and oleic acid (OA). CBD-NLCs were successfully prepared with an entrapment efficiency (E.E.) of 100%. All formulations showed particle sizes between 160 and 200 nm with PDIs less than 0.10. The type of surfactant and oil used affected the particle sizes, zeta potential, and crystallinity of the CBD-NLCs. CBD-NLCs stabilized with TG450 showed higher crystallinity after production and storage at 30 °C for 30 days as compared to those with P188. Encapsulation of the CBD extract in NLCs enhanced its chemical stability after exposure to simulated sunlight (1000 kJ/m2) compared to that of the CBD extract in ethanolic solution. The CBD-NLCs prepared from MCT and OA showed slower CBD release compared with that from Transcutol® P, and the kinetic data for release of CBD from CBD-NLCs followed Higuchi’s release model with a high coefficient of determination (>0.95). The extent of CBD permeation through Strat-M® depended on the oil type. The cytotoxicity of the CBD extract on HaCaT and HDF cells was reduced by encapsulation in the NLCs. The anti-inflammatory activity of the CBD extract in RAW264.7 cell macrophages was enhanced by encapsulation in CBD-NLCs prepared from MCT and OA.
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Liu, Zhidong, Shufang Nie, Hong Guo, Weisan Pan, and Jiawei Li. "Effects of Transcutol P on the corneal permeability of drugs and evaluation of its ocular irritation of rabbit eyes." Journal of Pharmacy and Pharmacology 58, no. 1 (2006): 45–50. http://dx.doi.org/10.1211/jpp.58.1.0006.
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Shakeel, Faiyaz, Mohsin Kazi, Fars K. Alanazi, and Prawez Alam. "Solubility of Cinnarizine in (Transcutol + Water) Mixtures: Determination, Hansen Solubility Parameters, Correlation, and Thermodynamics." Molecules 26, no. 22 (2021): 7052. http://dx.doi.org/10.3390/molecules26227052.
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Between 293.2 and 313.2 K and at 0.1 MPa, the solubility of the weak base, cinnarizine (CNZ) (3), in various {Transcutol-P (TP) (1) + water (2)} combinations is reported. The Hansen solubility parameters (HSP) of CNZ and various {(TP) (1) + water (2)} mixtures free of CNZ were also predicted using HSPiP software. Five distinct cosolvency-based mathematical models were used to link the experimentally determined solubility data of CNZ. The solubility of CNZ in mole fraction was increased with elevated temperature and TP mass fraction in {(TP) (1) + water (2)} combinations. The maximum solubility of CNZ in mole fraction was achieved in neat TP (5.83 × 10−2 at 313.2 K) followed by the minimum in neat water (3.91 × 10−8 at 293.2 K). The values of mean percent deviation (MPD) were estimated as 2.27%, 5.15%, 27.76%, 1.24% and 1.52% for the “Apelblat, van’t Hoff, Yalkowsky–Roseman, Jouyban–Acree, and Jouyban–Acree–van’t Hoff models”, respectively, indicating good correlations. The HSP value of CNZ was closed with that of neat TP, suggesting the maximum solubilization of CNZ in TP compared with neat water and other aqueous mixtures of TP and water. The outcomes of the apparent thermodynamic analysis revealed that CNZ dissolution was endothermic and entropy-driven in all of the {(TP) (1) + water (2)} systems investigated. For {(TP) (1) + water (2)} mixtures, the enthalpy-driven mechanism was determined to be the driven mechanism for CNZ solvation. TP has great potential for solubilizing the weak base, CNZ, in water, as demonstrated by these results.
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Yadav, Pankajkumar S., Ekta Yadav, Amita Verma, and Saima Amin. "Development, Characterization, and Pharmacodynamic Evaluation of Hydrochlorothiazide Loaded Self-Nanoemulsifying Drug Delivery Systems." Scientific World Journal 2014 (2014): 1–10. http://dx.doi.org/10.1155/2014/274823.
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The objective of the current work was to develop optimized self-nanoemulsifying drug delivery systems (SNEDDS) and evaluate theirin vitroandin vivoperformance. The research comprised various studies which includes solubility studies in various vehicles, pseudoternary phase diagram construction, and preparation and characterization of SNEDDS along within vitrodissolution andin vivopharmacodynamic profiling. Based on dissolution profile, a remarkable increase in rate of dissolution was observed in comparison with plain drug and marketed formulation. Optimized SNEDDS formulation was composed of Capmul MCM (19.17% w/w), Tween 80 (57.5% w/w), Transcutol P (12.7% w/w), and HCT (4.17% w/w).In vivopharmacodynamic evaluation in Wistar rats showed considerable increase in pharmacological effect of HCT by SNEDDS formulation as compared with plain HCT.
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Baboota, Sanjula, Faiyaz Shakeel, Alka Ahuja, Javed Ali, and Sheikh Shafiq. "Design, development and evaluation of novel nanoemulsion formulations for transdermal potential of celecoxib." Acta Pharmaceutica 57, no. 3 (2007): 315–32. http://dx.doi.org/10.2478/v10007-007-0025-5.
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Design, development and evaluation of novel nanoemulsion formulations for transdermal potential of celecoxibThe aim of the present study was to investigate the potential of nanoemulsion formulations for transdermal delivery of celecoxib (CXB). Thein vitroskin permeation profile of optimized formulations was compared with CXB gel and nanoemulsion gel. Significant increase in the steady state flux (Jss), permeability coefficient (Kp) and enhancement ratio (Er) was observed in nanoemulsion formulations T1 and T2 (p< 0.05). The highest value of these permeability parameters was obtained in formulation T2, which consisted of 2% (m/m) of CXB, 10% (m/m) of oil phase (Sefsol 218 and Triacetin), 50% (m/m) of surfactant mixture (Tween-80 and Transcutol-P) and 40% (m/m) water. The anti-inflammatory effects of formulation T2 showed a significant increase (p< 0.05) in inhibition after 24 h compared to CXB gel and nanoemulsion gel on carrageenan-induced paw edema in rats. These results suggested that nanoemulsions are potential vehicles for improved transdermal delivery of CXB.
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Sawant, Rutuja R. "FABRICATION AND EVALUATION OF ULTRADEFORMABLE VESICULAR NANOGEL LOADED WITH ECONAZOLE NITRATE." INDIAN DRUGS 62, no. 01 (2025): 28–34. https://doi.org/10.53879/id.62.01.14849.
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Transferosomes are advanced ultradeformable vesicles designed to enhance permeability across biological barriers. This study aimed to improve the efficacy of econazole nitrate by formulating transferosomes with edge activators to enhance drug release and penetration. They were prepared via thin-film hydration using econazole nitrate, soya lecithin, Tween®80, sodium deoxycholate and Span®60. The optimized Span®60 based formulation achieved an entrapment efficiency of 85.89 %, particle size of 63.8 nm, zeta potential of -31 mV, and a polydispersity index of 0.233. The drug when incorporated into 1 % Carbopol® 934 gel with Transcutol® P, demonstrated 89.11 % in vitro drug release and superior antifungal activity against Candida albicans compared to standard and plain econazole nitrate gels, highlighting improved release, penetration and therapeutic potential.
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Zhang, Hongyu, Jingwen Guo, Zhi Wang, Na Wang, Nianping Feng, and Yongtai Zhang. "Diethylene glycol monoethyl ether-mediated nanostructured lipid carriers enhance trans-ferulic acid delivery by Caco-2 cells superior to solid lipid nanoparticles." Acta Pharmaceutica 73, no. 1 (2023): 133–43. http://dx.doi.org/10.2478/acph-2023-0009.
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Abstract This work aimed to compare the performance of trans-ferulic acid-encapsulated nanostructured lipid carriers (NLCs) and solid lipid nanoparticles (SLNs) for transport by Caco-2 cells. The NLC particles (diameter: 102.6 nm) composed of Compritol® 888 ATO, ethyl oleate, Cremophor® EL, and Transcutol® P were larger than the SLNs (diameter: 86.0 nm) formed without liquid lipid (ethyl oleate), and the former had a higher encapsulation efficiency for trans-ferulic acid (p < 0.05). In vitro cultured Caco-2 cell transport was used to simulate intestinal absorption, and the cellular uptake of NLCs was higher than that of SLNs (p < 0.05). Compared to SLNs, NLCs greatly enhanced trans-ferulic acid permeation through the MillicellTM membrane (p < 0.05). This work confirms that NLCs have better properties than SLNs in terms of increasing drug transport by Caco-2 cells. This helps to comprehend the approach by which NLC-mediated oral bioavailability of trans-ferulic acid is better than that mediated by SLNs, as shown in our previous report.
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Vidyadhara, S., RLC Sasidhar, Y. A. Chowdary, K. L. Lavanya, and S. B. Lakshmi. "DESIGN AND EVALUATION OF ROSUVASTATIN SMEDDS FOR ENHANCING SOLUBILITY AND DISSOLUTION RATE." INDIAN DRUGS 53, no. 03 (2016): 40–46. http://dx.doi.org/10.53879/id.53.03.10136.
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The objective of present study was to improve solubility and dissolution rate of rosuvastatin by formulating it as a self micro emulsifying drug delivery system (SMEDDS). The SMEDDS were prepared by using capmul McM and capryol 90 as oils Polaxomer 407 as surfactant and Transcutol hP and Soluphor P as co-surfactants. The liquid SMEDDS were then converted into free flowing powder by adsorbing onto solid carriers like magnesium aluminium silicate. The prepared SMEDDs were further evaluated for particle size, phase separation, droplet size, drug content and for in vitro drug release. From the results, it was observed that the SMEDDs were found to be stable. Among the prepared SMEDDS the formulations prepared with oil to co-surfactant ratios of 1:3 showed highest rates of dissolution. The FTIR and DSc analysis on optimised formulations revealed that there were no major interactions between drug and excipients.
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Goyal, Urvash, Ritika Arora, and Geeta Aggarwal. "Formulation design and evaluation of a self-microemulsifying drug delivery system of lovastatin." Acta Pharmaceutica 62, no. 3 (2012): 357–70. http://dx.doi.org/10.2478/v10007-012-0022-1.
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Self-microemulsifying drug delivery system (SMEDDS) of lovastatin was aimed at overcoming the problems of poor solubility and bioavailability. The formulation strategy included selection of oil phase based on saturated solubility studies and surfactant and co-surfactant screening on the basis of their emulsification ability. Ternary phase diagrams were constructed to identify the self-emulsifying region. Capryol 90 (20 %) as oil, Cremophore RH40 (40 %) as surfactant and Transcutol P (40 %) as co-surfactant were concluded to be optimized components. The prepared SMEDDS was characterized through its droplet size, zeta potential, emulsification time, rheological determination and transmission electron microscopy. The optimized formulation exhibited 94 % in vitro drug release, which was significantly higher than that of the drug solution. In vivo studies using the Triton-induced hyperlipidemia model in Wistar rats revealed considerable reduction in lipid levels compared to pure lovastatin. The study confirmed the potential of lovastatin SMEDDS for oral administration.
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Shen, Meiyue, Chao Liu, Xiaocao Wan, Nabil Farah, and Liang Fang. "Development of a daphnetin transdermal patch using chemical enhancer strategy: insights of the enhancement effect of Transcutol P and the assessment of pharmacodynamics." Drug Development and Industrial Pharmacy 44, no. 10 (2018): 1642–49. http://dx.doi.org/10.1080/03639045.2018.1483391.
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Shakeel, Faiyaz, Nazrul Haq, Ibrahim Alsarra, and Sultan Alshehri. "Solubility Data, Solubility Parameters and Thermodynamic Behavior of an Antiviral Drug Emtricitabine in Different Pure Solvents: Molecular Understanding of Solubility and Dissolution." Molecules 26, no. 3 (2021): 746. http://dx.doi.org/10.3390/molecules26030746.
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The solubility values, various Hansen solubility parameters (HSPs) and thermodynamic behavior of emtricitabine (ECT) in twelve different pure solvents (PS) were estimated using various experimental as well as computational methods. Experimental solubility values (xe) of ECT in twelve different PS were obtained at T = 298.2 K to 318.2 K and p = 0.1 MPa. The xe values of ECT were correlated by “van’t Hoff, Apelblat and Buchowski-Ksiazaczak λh models”. Various HSPs for ECT and twelve different PS were also calculated using “HSPiP software”. The xe values of ECT were estimated maximum in polyethylene glycol-400 (PEG-400; 1.41 × 10−1), followed by ethylene glycol, Transcutol-HP, propylene glycol, methanol, water, isopropanol, ethanol, 1-butanol, dimethyl sulfoxide, 2-butanol and EA (1.28 × 10−3) at T = 318.2 K. “Apparent thermodynamic analysis” showed an “endothermic and entropy-driven dissolution” of ECT. Overall, PEG-400 was found as the best/ideal solvent for solubility/miscibility of ECT compared to other solvents studied.
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Ansari, Khalid Akhter, Kunal Pratap Pagar, Shoeb Anwar, and Pradeep Ratilal Vavia. "Design and optimization of self-microemulsifying drug delivery system (SMEDDS) of felodipine for chronotherapeutic application." Brazilian Journal of Pharmaceutical Sciences 50, no. 1 (2014): 203–12. http://dx.doi.org/10.1590/s1984-82502011000100021.
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The objective of this research work was to design, develop and optimize the self micro-emulsifying drug delivery system (SMEDDS) of Felodipine (FL) filled in hard gelatine capsule coated with polymer in order to achieve rapid drug release after a desired time lag in the management of hypertension. Microemulsion is composed of a FL, Lauroglycol FCC, Transcutol P and Cremophor EL. The optimum surfactant to co-surfactant ratio was found to be 2:1. The resultant microemulsions have a particle size in the range of 65-85 nm and zeta potential value of -13.71 mV. FL release was adequately adjusted by using pH independent polymer i.e. ethyl cellulose along with dibutyl phthalate as plasticizer. Influence of formulation variables like viscosity of polymer, type of plasticizer and percent coating weight gain was investigated to characterize the time lag. The developed formulation of FL SMEDDS capsules coated with ethyl cellulose showed time lag of 5-7 h which is desirable for chronotherapeutic application.
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Sabir, Fakhara, Gábor Katona, Ruba Ismail, Bence Sipos, Rita Ambrus, and Ildikó Csóka. "Development and Characterization of n-Propyl Gallate Encapsulated Solid Lipid Nanoparticles-Loaded Hydrogel for Intranasal Delivery." Pharmaceuticals 14, no. 7 (2021): 696. http://dx.doi.org/10.3390/ph14070696.
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The objective of the present study was to develop n-propyl gallate-loaded solid lipid nanoparticles (PG-SLNs) in a hydrogel (HG) formulation using Transcutol-P (TC-P) as a permeation enhancer. Modified solvent injection technique was applied to produce optimized PG-SLNs via the Quality by Design approach and central composite design. The in vitro mucoadhesion, scavenging activity, drug release, permeation studies of PG from PG-SLNs-loaded HG were evaluated under simulated nasal conditions. Compared with in vitro release behavior of PG from SLNs, the drug release from the PG-SLNs-loaded HG showed a lower burst effect and sustained release profile. The cumulative permeation of PG from PG-SLNs-loaded HG with TC-P was 600 μg/cm2 within 60 min, which is 3–60-fold higher than PG-SLNs and native PG, respectively. Raman mapping showed that the distribution of PG-SLNs was more concentrated in HG having lower concentrations of hyaluronic acid. The scavenging assay demonstrated increased antioxidant activity at higher concentrations of HG. Due to enhanced stability and mucoadhesive properties, the developed HG-based SLNs can improve nasal absorption by increasing residence time on nasal mucosa. This study provides in vitro proof of the potential of combining the advantages of SLNs and HG for the intranasal delivery of antioxidants.
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Shakeel, Faiyaz, Nazrul Haq, and Sultan Alshehri. "Solubility Data of the Bioactive Compound Piperine in (Transcutol + Water) Mixtures: Computational Modeling, Hansen Solubility Parameters and Mixing Thermodynamic Parameters." Molecules 25, no. 12 (2020): 2743. http://dx.doi.org/10.3390/molecules25122743.
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The solubility values and thermodynamic parameters of a natural phytomedicine/nutrient piperine (PPN) in Transcutol-HP (THP) + water combinations were determined. The mole fraction solubilities (xe) of PPN in THP + water combinations were recorded at T = 298.2–318.2 K and p = 0.1 MPa by the shake flask method. Hansen solubility parameters (HSPs) of PPN, pure THP, pure water and THP + water mixtures free of PPN were also computed. The xe values of PPN were correlated well with “Apelblat, Van’t Hoff, Yalkowsky–Roseman, Jouyban–Acree and Jouyban–Acree–Van’t Hoff” models with root mean square deviations of < 2.0%. The maximum and minimum xe value of PPN was found in pure THP (9.10 × 10−2 at T = 318.2 K) and pure water (1.03 × 10−5 at T = 298.2 K), respectively. In addition, HSP of PPN was observed more closed with that of pure THP. The thermodynamic parameters of PPN were obtained using the activity coefficient model. The results showed an endothermic dissolution of PPN at m = 0.6–1.0 in comparison to other THP + water combinations studied. In addition, PPN dissolution was recorded as entropy-driven at m = 0.8–1.0 compared with other THP + water mixtures evaluated.
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Shrivastava, Nupur, Ankit Parikh, Rikeshwer Prasad Dewangan, et al. "Solid Self-Nano Emulsifying Nanoplatform Loaded with Tamoxifen and Resveratrol for Treatment of Breast Cancer." Pharmaceutics 14, no. 7 (2022): 1486. http://dx.doi.org/10.3390/pharmaceutics14071486.
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The solid self-nanoemulsifying drug delivery system (s-SNEDDS) is a growing platform for the delivery of drugs via oral route. In the present work, tamoxifen (TAM) was loaded in SNEDDS with resveratrol (RES), which is a potent chemotherapeutic, antioxidant, anti-inflammatory and P-gp inhibitor for enhancing bioavailability and to obtain synergistic anti-cancer effect against breast cancer. SNEDDS were developed using capmul MCM as oil, Tween 80 as surfactant and transcutol-HP as co-surfactant and optimized by central composite rotatable design. Neusilin US2 concentration was optimized for adsorption of liquid SNEDDS to prepare s-SNEDDS. The developed formulation was characterized and investigated for various in vitro and cell line comparative studies. Optimized TAM-RES-s-SNEDDS showed spherical droplets of a size less than 200 nm. In all in vitro studies, TAM-RES-s-SNEDDS showed significantly improved (p ˂ 0.05) release and permeation across the dialysis membrane and intestinal lumen. Moreover, TAM-RES-s-SNEDDS possessed significantly greater therapeutic efficacy (p < 0.05) and better internalization on the MCF-7 cell line as compared to the conventional formulation. Additionally, oral bioavailability of TAM from SNEDDS was 1.63 folds significantly higher (p < 0.05) than that of combination suspension and 4.16 folds significantly higher (p < 0.05) than TAM suspension. Thus, findings suggest that TAM- RES-s-SNEDDS can be the future delivery system that potentially delivers both drugs to cancer cells for better treatment.
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Singh, Gurpreet, Nisha Rawat, Kirti Singh, Amita Sarwal, and V. R. Sinha. "INVESTIGATING THE POTENTIAL OF AN ANTIDEPRESSANT INTRANASAL MUCOADHESIVE MICROEMULSION." International Journal of Pharmacy and Pharmaceutical Sciences 10, no. 6 (2018): 125. http://dx.doi.org/10.22159/ijpps.2018v10i6.25710.
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Objective: The main aim of this study was to formulate, develop and optimized a duloxetine hydrochloride (dlx-hcl) loaded mucoadhesive microemulsion intended for intranasal administration.Methods: Established on solubility studies capmul mcm, transcutol-p, labrasol were used as oil, co-surfactant and surfactant respectively. The optimized mucoadhesive microemulsion prepared using water titration method was further characterized for particle size, polydispersity index, zeta potential and conductivity measurements followed by drug content, nasal cilio toxicity and biochemical estimation of the selected formulation.Results: All physicochemical parameters conducted, proved that dlx-hcl microemulsion was appropriate for nasal delivery. Chitosan, used as mucoadhesive polymer demonstrated enhanced retention time of the microemulsion in nasal mucosa with no signs of toxicity and epithelial damage. The particle size and zeta potential were found to be of 200 nm and-15 mV respectively considering the formulation safe for nasal delivery.Conclusion: This formulation strategy can be used as an effective targeting technique for the drugs having low bioavailability and poor brain penetration along with an effective method for the treatment long-term disease like depression.
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Suthar, V., M. Gokel, S. Butani, and A. Solanki. "SELF-EMULSIFYING DRUG DELIVERY SYSTEM CONTAINING ACECLOFENAC: DESIGN & DEVELOPMENT USING QUALITY BY DESIGN (QBD) CONCEPT." INDIAN DRUGS 51, no. 06 (2014): 16–26. http://dx.doi.org/10.53879/id.51.06.p0016.
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The aim of the present study was to develop self-emulsifying drug delivery system (SEDDS) of aceclofenac for potential improvement in the in vitro dissolution. The Food and Drug Control Agency (FDCA) has put more stress on the quality, safety and efficacy of the dosage form. The use of design of experiments and quality by Design (QbD) in the development of self emulsifying drug delivery system (SEDDS) containing aceclofenac is demonstrated. The optimum formulation contained Labrafil M 1944 CS, Tween 80 and Transcutol P. The systematic approach enabled us in identifying the design space. The results revealed that while devising the control strategies during manufacturing, more attention should be focused on the ratios of oil to surfactant and surfactant to co-surfactant. The drug was released at a faster rate due to a large surface area. The current approach enabled us to develop a dosage form which is economic, patient-friendly and does not require assistance of a doctor or nurse, especially at remote places at odd hours.
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Nguyen, Van Hong, Mai Chau Ngoc Nguyen, and Huyen Thi Trang Nguyen. "Berberine nanostructured lipid carriers by ultrasonication technique: initial study for skin and oral administration." Advances in Natural Sciences: Nanoscience and Nanotechnology 16, no. 1 (2024): 015002. https://doi.org/10.1088/2043-6262/ada002.
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Abstract Berberine (BBR), a natural bioactive ingredient from Eastern nations, has low solubility and permeability that limits its applications. Hence, berberine nanostructured lipid carriers (BBR-NLCs) were fabricated to improve the drug therapeutic effectiveness. Glycerol monostearate, stearic acid and oleic acid were chosen for lipid base whereas Pluronic F127, Span 80, and Transcutol-P were used as the surfactant and co-surfactant. BBR-NLCs had an average particle size of 82 nm, zeta potential of −32 mV, and narrow size distribution (PDI approximately 0.2), prepared with probe ultrasonication at 490 W in 15 min. In addition, BBR-NLCs prepared at optimized conditions showed around 92% of encapsulation efficiency with drug loading over 5.5%. NLCs presented sustained released through mouse skin, dialysis membrane in Franz cell model, and oral dissolution test, compared with free drug over 24 h. Moreover, blank NLCs even increased the cell viability of HaCaT and HEK293T cells at lower concentrations. NLCs significantly enabled higher interactive BBR quantity with investigated cells. Therefore, BBR-NLCs could be considered as a potential nanocarrier for improved bioavailability of this therapeutic agent.
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Gupta, Sudhir, and Kamal Singh Rathore. "Formulation and Evaluation of Novel Lipid-Based Nanocarriers for Targeted Ocular Delivery of Prednisolone Acetate." Journal of Neonatal Surgery 14, no. 17S (2025): 36–51. https://doi.org/10.63682/jns.v14i17s.4469.
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Objective: In the present research work, the aim was to prepare and evaluate prednisolone acetate solid lipid nanoparticles at eye surface for the treatment of ocular inflammation. Methods: Solid lipid nanoparticles were prepared by high pressure homogenization followed by probe sonication. The amounts of polymers were selected on the basis of optimum quantity required for sustained release of drugfrom preparation and as reported in literature and performed ranging study. Results and discussion: Glyceryl monostearate, Tween 80 and transcutol P were used as solid lipid, surfactant and co-surfactant respectively. All formulation was evaluated for particle size, zeta potential, entrapment efficiency % drug content and release study. Nine formulations for each approach were prepared and optimized successfully using 32 factorial designs. Optimization was done by DoE software version Version 13.0.10.064. Conclusion: Solid lipid nanoparticles were successfully developed using high pressure homogenization method. Results of the various parameters indicated that prednisolone acetate can be formulated into nanoparticles using GMS thereby improving its ocular permeability. Stability studies indicated no change in coloration or any other physical parameters.