Objective: The present study is focused on optimization of elastic liposomes-in-vehicle formulations in respect to drug release and formulation properties. By combining penetration potential of elastic liposomes containing high ratio of entrapped drug and physicochemical properties of vehicles, both affecting the release and texture properties, optimal formulation could be achieved.
Materials and methods: Deformable, propylene glycol-containing or conventional liposomes with hydrophilic model drug (diclofenac sodium) were incorporated into the following vehicles appropriate for skin application: a hydrogel, a cream base and derma membrane structure base cream (DMS base). Each formulation was assessed for in vitro drug release and mechanical properties.
Results and discussion: The composition and type of both liposomes and the vehicle affected the rate and amount of the released drug. The cream base exhibited the slowest release, followed by the hydrogel and DMS base. Similar release profiles were achieved with both types of elastic vesicles (deformable and propylene glycol liposomes); the slowest release was observed for conventional liposomes, regardless of the vehicle used. The drug release profiles from different liposomes-in-vehicle formulations were in agreement with the physicochemical properties of the formulations. All of the liposomes were found to be compatible with the hydrogel preserving its original textures, whereas a significant decrease in all texture parameters was observed for liposomes-in-DMS base, regardless of liposome type.
Conclusion: Propylene glycol liposomes-in-hydrogel is considered as the optimal formulation for improving skin delivery of hydrophilic drug. Further investigations involving in vivo animal studies are necessary to confirm its applicability in skin therapy. 相似文献
Objective: To compare various solubilizing agents for their solubilizing propensity as well as effect of pH, concentration and time on solubility of a highly hydrophobic drug.Materials and methods: Dendrimers were synthesized by divergent method. Solubilization studies were carried out at different pH, concentration and time using Paclitaxel (PTX) as model drug. Hemolytic toxicity study was also performed.Results: The solubility of PTX was increased with increasing concentration of solubilizing agents and the order of solubility enhancement effect of different solubilizing agents was found to be in the following order: fifth generation (5.0?G) poly(propylene imine) (PPI) dendrimers?>?β-CD?>?Tween 80?>?polyethylene glycol 6000. The solubility of PTX was found to be highest at pH 5.0 followed by pH 7.4 than pH 9.2. The result of hemolytic toxicity studies displayed that when these solubilizing agents are given in combination with PTX, the toxicity was found to be reduced as compare to plain drug.Conclusions: The solubility of PTX was found to be significantly higher in the presence of 5.0?G PPI dendrimers as compared to the other solubilizing agents. It is also concluded that 5.0?G PPI dendrimers not only enhanced the solubility of PTX many folds but also reduced the toxicity of PTX. 相似文献
Context: Transdermal spray (TS) of clotrimazole (CTZ) was formulated to improve the drug transport through the skin up to 12?h to achieve the antifungal efficacy.Objective: The aim of present study was to formulate and evaluate antifungal transdermal spray to improve the permeation of clotrimazole across the skin and to decrease the dosing frequency in fungal infection.Materials and methods: Different ratios of ethanol and acetone and various grades of eudragit and ethyl cellulose were evaluated according to six criteria: viscosity, drying time, stickiness, appearance and integrity on skin and water washability. Propylene glycol (PG) and polyethylene glycol 400 (PEG 400) were used in the study as plasticizer and solubilizer. The TS was evaluated for in vitro drug release, spray angle, spray pattern, average weight per dose, pH, drug content, evaporation time, leak test and antifungal efficacy study.Results and discussion: Eudragit E100 and blend of ethanol and acetone (80:20) satisfied the desired criteria. The selection of optimized batch was based on the results of in vitro drug release, spray pattern and spray angle. The optimized batch showed the spray angle <85° and uniform spray pattern. The formulation containing PG showed higher drug release than PEG 400. The inclusion of eutectic mixture consisting of camphor and menthol (1:1) showed improved drug transport through the rat skin and larger mean zone of inhibition indicating the improved antifungal efficacy.Conclusion: The TS of CTZ can be an innovative and promising approach for the topical administration in the fungal diseases. 相似文献
Forty-five multiparous Holstein cows were assigned to one of 3 treatments in a randomized complete block design. The objective was to evaluate the effects of sodium monensin (M) and propylene glycol (PPG) during the prepartum period on performance and metabolic parameters during the late dry and first 9 wk postpartum for cows receiving M postpartum. Treatments were: control (C), M in a controlled-release capsule to deliver 335 +/- 33 mg/d for approximately 100 d, and 300 mL/d of PPG drenched orally. Treatments started at 35 and 21 d prior to the expected date of calving for cows receiving M and PPG, respectively. To ensure that all treatments would be restricted to the prepartum period, C and PPG cows received a M controlled-release capsule in the first 24 h after calving. Prepartum propylene glycol administration increased concentrations of glucose and insulin, and decreased beta-hydroxybutyrate and nonesterified fatty acids in plasma prepartum. Milk production was similarly affected by treatments. However, prepartum M treated cows tended to produce more 3.5% fat-corrected milk compared with control, but similar to PPG. Milk fat content and yield tended to be greater for cows that received M prepartum than for C cows, while PPG cows were similar to M and C. Prepartum administration of M decreased milk protein content, but no effect was observed on protein yield. 相似文献