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In past years, various studies have considered transdermal drug delivery system for improving patient compliance. One approach to deliver drug via transdermal route is transdermal patch. These patches include single-layer drug in adhesive patches and micro reservoir transdermal patch & matrix system. Acrylic-acid, hydroxypropyl methylcellulose (HPMC) and polyethylene glycol are commonly used polymers for manufacturing of transdermal patches. Characterization of patches includes patch thickness, weight uniformity, irritation studies, in-vitro drug release and permeation studies. This review summarizes various polymers, types of transdermal patches and evaluation of transdermal patches based on up-to-date data extracted from reputed journals and official websites. [ABSTRACT FROM AUTHOR]

Wound healing faces significant challenges in clinical settings. It often contains a series of dynamic and complex physiological healing processes. Instead of creams, ointments and solutions, alternative treatment approaches are needed. The main objective of the study was to formulate bacitracin zinc-loaded topical patches as a new therapeutic agent for potential wound healing. A free radical polymerization technique was optimized for synthesis. Polyethylene glycol-8000 (PEG-8000) was chemically cross-linked with acrylic acid in aqueous medium, using Carbopol 934 as a permeation enhancer and tween 80 as surfactant. Ammonium persulfate and N,N'-Methylenebisacrylamide (MBA) were utilized as initiator and cross-linker. FTIR, DSC, TGA, and SEM were performed, and patches were evaluated for swelling dynamics, sol-gel analysis, in vitro drug release in various media. A Franz diffusion cell was used for the permeation study. Irritation and wound healing with the drug-loaded patches were also studied. The characterization studies confirmed the formation of a cross-linked hydrogel network. The highest swelling and drug release were observed in formulations containing highest Polyethylene glycol-8000 and lowest N,N'-Methylenebisacrylamide concentrations. The pH-sensitive behavior of patches was also confirmed as more swelling, drug release and drug permeation across skin were observed at pH 7.4. Fabricated patches showed no sign of irritation or erythema as evaluated by the Draize scale. Faster wound healing was also observed with fabricated patches compared to marketed formulations. Therefore, such a polymeric network can be a promising technology for speeding up wound healing and minor skin injuries through enhanced drug deposition. [ABSTRACT FROM AUTHOR]

Objectives: The present study was aimed to develop itraconazole (ITZL)-loaded NLC for the treatment of fungal infection. Methods: The formulation was prepared and optimized by the hot homogenization method and Box-Behnken statistical design. The total lipid ratio (A), surfactant (B), and homogenization cycle (C) were selected as independent variables, and the effects of variables were evaluated on particle size (R1), entrapment efficiency (R2), and drug release in 12 h (R3). Results: The optimized formulation ITZLNLCopt showed particle size (147.31 ± 1.43 nm) high entrapment efficiency (86.36 ± 0.83%) and drug release (77.23 ± 3.33 %). The formulation ITZLNLCopt converted to carbopol (1% w/v) based gel (ITZLNLCopt gel) and showed good consistency and spreadability. The formulation ITZLNLCopt gel showed higher drug release (88.43 ± 2.54 % up to 24 h) and flux (2.46 fold) than control gel. The zone of inhibition results showed 2.6 and 2.36 fold higher inhibition (P < 0.05) than control gel (ITZL gel) against Candida albicans and Aspergillus fumigatus. Conclusions: It could be concluded that ITZLNLC gel as a potential alternative for the treatment of topical fungal infection after clinical study in the future. [ABSTRACT FROM AUTHOR]

The objective of research work was to improve the permeability of Ketoprofen and to provide controlled release of drug to provide maximum effective concentration. Transdermal drug delivery systems are polymeric patches containing dissolved or dispersed drugs that deliver therapeutic agents at a constant rate to the human skin. Matrix type transdermal patches containing Ketoprofen were prepared by solvent casting method employing aluminium foil method. Polyethylene glycol (PEG) 400 was used as plasticizer and Dimethyl sulfoxide (DMSO) was used as penetration enhancer. Polymers were selected on the basis of its adhering and non-toxic property. Drug polymer interactions determine by FTIR and standard calibration curve of Ketoprofen were determine by using UV estimation. Transdermal patch was prepared by using HPMC K-4 M: PVP K-30, HPMC K-15 M: PVP K-30, HPMC K-100 M: PVP K-30, Eudragit RS-100:PVP K-30 showed good physical properties. All prepared formulations indicated good physical stability. In-vitro drug permeation studies of formulations were performed by using Franz diffusion cells using abdomen skin of Wistar albino rat. Result, showed best in-vitro skin permeation through rat skin (Wistar albino rat) as compared to all other formulations prepared with hydrophilic polymer containing permeation enhancer. The permeability of Ketoprofen was increased with increase in PVP content. The burst effect due to the incorporation of PVP was because of the rapid dissolution of the surface hydrophilic drug which gets swell and thus leads to the decrease of mean diffusion path length of the drug molecules to permeate into dissolution medium and higher permeation rates. [ABSTRACT FROM AUTHOR]

The aim of the present investigation was to formulate and evaluate topical calcineurin inhibitor loaded transfersomal drug delivery for vitiligo using rota evaporator followed by thin film method. Tacrolimus can restore the melanocytes if given in transfersomal gel. Fourier transform infrared spectroscopy (FTIR) had employed to study drug-excipients incompatibility. Analytical method was performed using UV spectrophotometer. Topical calcineurin inhibitor loaded transfersomal gel was evaluated for particle size, zeta potential, percent drug entrapment, surface morphology, in-vitro drug release study, in vitro permeability study and stability study. Optimization of process parameter was done by 3² full factorial Design Expert software. Topical calcineurin inhibitor was successfully prepared with drug:lipid(1:10), lipid:surfactant(9:1), water as hydration medium, chloroform:methanol(9:1) as solvent, HPMCK100 as mucoadhesive agent and extract of catechu powder to provide colour on skin. Optimization study of process parameter shows that batch prepared with hydration time 55 min, evaporation time 15 min, hydration temperature is 50°C and temperature to form thin film is 60°C as optimum condition for rota evaporator. Particle size, zeta potential, percent drug entrapment were found to be 155.5 nm, -49 mV, 80% respectively for optimized batch. [ABSTRACT FROM AUTHOR]

A microemulsion system containing Thai mango seed kernel extract (MSKE, cultivar “Fahlun”) was developed and characterised for the purpose of topical skin delivery. The MSKE-loaded microemulsions were prepared by using the spontaneous emulsification method. Isopropyl myristate (IPM) was selected as the oil phase. A polyoxyethylene sorbitan monooleate and sorbitan monododecanoate (1:1, w/w) system was used as the surfactant phase; an aqueous mixture of different cosurfactants (absolute ethanol, 96.3% v/v ethanol, 1-propanol, 2-propanol or 1,2-propanediol) at a weight ratio of 1:1 was used as the aqueous phase. Among the cosurfactants studied, the 1-propanol aqueous mixture had the largest microemulsion region (48.93%) in the pseudo-ternary phase diagram. Microemulsions containing 1% MSKE demonstrated good physicochemical stability during a six-month study period at 25 ± 2 °C/60% ± 5% RH. The ex vivo skin permeation study demonstrated that the microemulsions exhibited a potent skin enhancement effect allowing MSKE to penetrate skin layers up to 60-fold higher compared with the control. Neither skin irritation nor skin corrosion was observed in ex vivo studies. The present study revealed that IPM-based microemulsion systems may be promising carriers to enhance skin penetration and delivering MSKE for topical treatment.

The aim of this study was to develop a Transdermal patch containing Cinnarizine using different ratios of hydrophilic and hydrophobic polymeric systems by solvent evaporation technique employing Polyethylene glycol (PEG 400) as plasticizer. The physicochemical compatibility of the drug and the polymers were studied by performing FT-IR spectroscopic analysis. Formulated patches were evaluated for physicochemical properties, skin irritation, in vitro drug release, ex-vivo permeation studies across rat abdominal skin and stability studies. The results of FT-IR studies revealed that there were no interactions between drug and polymers used. All the formulations exhibited uniformity in physicochemical properties. In vitro permeation studies of the formulations were performed by using Franz diffusion cells. Formulation F3 showed better permeation through rat skin (i.e., 8527.5±1.25μg/cm² /hr) compared to rest of formulations and followed Fick's diffusion mechanism. On the basis of in-vitro drug release and ex-vivo skin permeation performance, Formulation F3 containing the polymeric blend 19:1 Hydroxypropylmethyl Cellulose (HPMC E 50cps: Eudragit RL 100) has shown optimum release in comparison to other formulations and indicated good physical stability. So it has been demonstrated that Cinnarizine can be designed as matrix type transdermal drug delivery system (TDDS) and further in-vivo evaluations were required. [ABSTRACT FROM AUTHOR]

The objective of this study was to develop and evaluate a novel microemulsion based gel formulation containing tazarotene for targeted topical therapy of acne. Psudoternary phase diagrams were constructed to obtain the concentration range of oil, surfactant, and co-surfactant for microemulsion formation. The optimized microemulsion formulation containing 0.05% tazarotene was formulated by spontaneous microemulsification method consisting of 10% Labrafac CC, mixed emulsifiers 15% Labrasol–Cremophor–RH 40 (1:1), 15% Capmul MCM, and 60% distilled water (w/w) as an external phase. All plain and tazarotene-loaded microemulsions were clear and showed physicochemical parameters for desired topical delivery and stability. The permeation profiles of tazarotene through rat skin from optimized microemulsion formulation followed the Higuchi model for controlled permeation. Microemulsion-based gel was prepared by incorporating Carbopol®971P NF in optimized microemulsion formulation having suitable skin permeation rate and skin uptake. Microemulsion-based gel showed desired physicochemical parameters and demonstrated advantage over marketed formulation in improving the skin tolerability of tazarotene indicating its potential in improving its topical delivery. The developed microemulsion-based gel may be a potential drug delivery vehicle for targeted topical delivery of tazarotene in the treatment of acne. [ABSTRACT FROM PUBLISHER]

Objectives: The chief objective of the present research was to reduce local side effects by reducing the dose, controlling the release, and improving the stability by developing and optimizing tretinoin (TRT)-loaded topical emulgel formulation., Methods: TRT emulgel (TE) was prepared and optimized at varying ratios of excipients and using 3 2 optimal response surface design (ORSD). The TRT emulgel was optimized based on TRT content and in vitro release profile of TRT from formulated emulgel batches. The optimized TRT was characterized for physical properties, pH, viscosity, spreadability, extrudability, photomicroscopy, in vitro anti-acne, in vivo skin irritation, in vivo anti-inflammatory activity, and stability study., Results: The FTIR and DSC analysis revealed the compatibility between TRT and formulation excipients of emulgel. The batch F5 of emulgel formulation displayed maximum drug content (98.69±1.26%), and controlled TRT release (78.27±0.69%). Thus, batch F5 was selected as an optimized batch for further characterization. The photomicroscopic analysis of optimized TE exhibited the presence of spherical globules. The pH and viscosity of optimized TE were found to be 6.20±0.12 and 3240cP respectively. Besides, the optimized TE showed good spreadability and extrudability. The in vitro anti-acne activity against Propionibacterium acne (P. acne) of optimized TE (diameter of zone of inhibition 34.54±0.26mm) was found to be the comparatively same as that of marketed Sotret® gel (diameter of zone of inhibition 36.13±0.43mm). Moreover, no sign of irritation was observed in rats treated with optimized TE indicating the safety of TE. Furthermore, the optimized TE displayed significant (p<0.01) in vivo anti-inflammatory activity when compared to marketed gel. Besides, optimized TE was found to be stable when stored in cool conditions for three months., Conclusion: Thus, the emulgel could be a promising approach for the topical delivery of TRT with improved performance and reduced side effects., (Copyright © 2021 Académie Nationale de Pharmacie. Published by Elsevier Masson SAS. All rights reserved.)