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OBJECTIVE: To prepare a vardenafil cross-linked hydrogel patch and evaluate its quality characteristics. METHODS: The vardenafil cross-linked hydrogel patch was prepared by using sodium polyacrylate as the basic matrix material and aluminum hydroxide as the crosslinking agent, which was compared on transdermal permeation properties in vitro with vardenafil hydrochloride cross-linked patch and vardenafil hydrochloride gel. Transdermal permeation properties and drug content were determined by transdermal diffusion cell and HPLC. Then adhesive force was evaluated by initial adhesion tester, adhesion tester and peel tester. Besides, deformation resistance with moisture, heat and cold resistance, formability and skin irritation were also investigated. RESULTS: The vardenafil cross-linked hydrogel patch was a transparent and gelatinous solid with suitable viscidity. The method of content determination was validated in accordance with the requirements. The in vitro permeation rate of vardenafil cross-linked hydrogel patch fitted the zero-order release realation, and its permeation rate was higher than rates of vardenafil hydrochloride cross-linked patch and vardenafil hydrochloride gel in 24 h. And the cross-linked patch has better deformation resistance with moisture, heat and cold resistance, formability and no skin irritation. CONCLUSION: The vardenafil cross-linked hydrogel patch has good transdermal permeation properties and vardenafil is more suitable for transdermal delivery system than vardenafil hydrochloride, which provides theoretical and practical references for further research.
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ABSTRACT Natural latex from Hevea brasiliensis (Wild. ex A.Juss) Müll.Arg., Euphorbiaceae, showed angiogenic action and Casearia sylvestris Sw., Salicaceae, leaf derivatives presented anti-inflammatory and wound healing activities. Therefore, an association of these effects was interesting for wound healing applications. The aims of this study were the development of membranes of natural latex incorporated with C. sylvestris leaf derivatives (ethanolic extract, diterpene concentrated fraction and casearin J), their chemical and physical characterization, and the evaluation of in vitro skin permeation and retention of C. sylvestris bioactive secondary metabolites (diterpenes and phenolic compounds). The membranes were developed mixing hydroethanolic solutions of C. sylvestris derivatives with latex and drying them in a desiccator. They were characterized by infrared spectroscopy, scanning electron microscopy, water vapor permeability and mechanical resistance assays, demonstrating that all membranes were permeable, resistant and homogeneous in surfaces. The permeation and retention assays demonstrated dermal penetration of phenolic compounds for ethanolic extract membrane and of casearin-like clerodane diterpenes for all membranes, indicating that these membranes have great potential for therapeutical application as a topical system for C. sylvestris components releasing.
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OBJECTIVE:To compare in vivo and in vitro permeation behaviors of the ethosome gels of testosterone,testoster-one propionate and testosterone undecanoate. METHODS:The ethosome gels of testosterone,testosterone propionate and testoster-one undecanoate were prepared. With cumulative permeating amount and permeation rate as the indexes,Franz diffusion cell and HPLC were employed to compare in vitro permeation behaviors of 3 kinds of ethosome gels in mouse skin. With testosterone patch as the positive control drug, electrochemistry method was adopted to detect the concentration of testosterone in plasma 0,3,6, 9,12,24,36 and 48 h after applying such 3 kinds of ethosome gels on the back of rats,and then pharmacokinetic parameters were calculated with DAS 2.0 software. RESULTS:24 h cumulative permeating amounts of the ethosome gels of testosterone,tes-tosterone propionate and testosterone undecanoate were(234.31±13.8),(175.63±41.1)and(72.60±15.3)μg/cm2,and the per-meation rates were(10.25±1.9),(7.64±1.4)and(2.96±0.8)μg/(cm2·h),respectively. The pharmacokinetic parameters of the above-mentioned three kinds of ethosome gels and the positive control drug were respectively as follows as cmax of(20.19±2.57), (17.50±2.91),(0.23±0.04),(14.97±2.12)ng/ml,t1/2Ka of(2.80±0.45),(3.36±0.59),(4.02±0.62),(4.20±0.71)h,AUC0-48 h of(13.85±1.96),(13.93±2.13),(0.35±0.07),(11.76±2.31)ng·h/ml. CONCLUSIONS:in vivo and in vitro permeation behav-iors of the ethosome gels of testosterone and testosterone propionate are fairly good.
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Trandolapril is an antihypertensive agent which undergoes extensive first pass metabolism making it a possible candidate for transdermal delivery. Patches were prepared using hydroxypropylmethylcellulose, eudragit RL 100, gantrez and carbopol. The results of FTIR and DSC revealed no interaction between drug and polymers. The loss of moisture and uptake of moisture were within the limits. The formulations showed an extended release of the drug upto period of 24 hours during in vitro permeation studies and showed non-Fickian drug release. Stability of the optimized formulation was investigated as per ICH guidelines and was found to be stable with respect to drug content and in vitro permeation.
ABSTRACT
The main objective of the present study was to develop matrix-moderated transdermal systems of Indomethacin using various proportions of Ficus carica fruit mucilage. Physical evaluation was performed such as moisture content, moisture uptake, tensile strength, flatness and folding endurance. In-vitro permeation studies were performed in a Keshary-Chien diffusion cell. The matrix-type transdermal systems were prepared using Indomethacin with Ficus carica fruit mucilage by the solvent evaporation technique. The interactions between Indomethacin and Ficus carica fruit mucilage were performed. The transdermal patches were subjected to various physicochemical parameters viz., mechanical properties, permeation studies and skin irritation studies. The prepared patches possessed satisfactory pre-formulary and formulary characteristics. In vitro permeation studies were performed using a Keshary-Chien diffusion cell across hairless Albino rat skin. The non-ionic surfactants Span 80, Glycerin, Propylene glycol in the formulation played a role as permeability enhancer. The patches were seemingly free of potentially hazardous skin irritation. The experimental results shows that the release of drug from the patch delayed in controlled manner as the proportion of Ficus carica increased. It was concluded that Indomethacin can be developed as a transdermal patches with Ficus carica fruit mucilage.