Mortazavi Seyed Alireza, Pishrochi Sanaz, Jafari Azar Zahra
Department of Pharmaceutics, School of Pharmacy, Shahid Beheshti University of Medical Sciences, Tehran, Iran.
Department of Pharmaceutics, Pharmaceutical Sciences Branch, Islamic Azad University, Tehran, Iran.
Iran J Pharm Res. 2013 Fall;12(4):599-609.
In this study, tretinoin microemulsion has been formulated based on phase diagram studies by changing the amounts and proportions of inactive ingredients, such as surfactants, co-surfactants and oils. The effects of these variables have been determined on microemulsion formation, particle size of the dispersed phase and release profile of tretinoin from microemulsion through dialysis membrane. In released studies, static Franz diffusion cells mounted with dialysis membrane were used. Sampling was conducted every 3 h at room temperature over a period of 24 h. The amount of released drug was measured with UV-spectrophotometer and the percentage of drug released was calculated. Based on the results obtained, the oil phase concentration had a proportional effect on particle size which can consequently influence on drug release. The particle size and the amount of released drug were affected by the applied surfactants. The components of the optimized microemulsion formulation were 15% olive oil, 12% propylene glycol (as co-surfactant), 33% Tween(®)80 (as surfactant) and 40% distilled water, which was tested for viscosity and rheological behavior. The prepared tretinoin microemulsion showed pseudoplastic-thixotropic behavior. The profile of drug release follows zero order kinetics. The optimized tretinoin microemulsion showed enhanced in-vitro release profile compared to the commercial gels and creams.
在本研究中,基于相图研究,通过改变诸如表面活性剂、助表面活性剂和油等非活性成分的用量和比例,制备了维甲酸微乳。已确定这些变量对微乳形成、分散相粒径以及维甲酸通过透析膜从微乳中的释放曲线的影响。在释放研究中,使用安装有透析膜的静态弗兰兹扩散池。在室温下,于24小时内每隔3小时进行一次取样。用紫外分光光度计测量释放药物的量,并计算药物释放百分比。基于所得结果,油相浓度对粒径有正比效应,进而可影响药物释放。所应用的表面活性剂会影响粒径和药物释放量。优化后的微乳制剂成分包括15%橄榄油、12%丙二醇(作为助表面活性剂)、33%吐温80(作为表面活性剂)和40%蒸馏水,并对其粘度和流变行为进行了测试。所制备的维甲酸微乳表现出假塑性-触变性行为。药物释放曲线符合零级动力学。与市售凝胶和乳膏相比,优化后的维甲酸微乳显示出增强的体外释放曲线。