Pajić Nataša Z Bubić, Todosijević Marija N, Vuleta Gordana M, Cekić Nebojša D, Dobričić Vladimir D, Vučen Sonja R, Čalija Bojan R, Lukić Milica Ž, Ilić Tanja M, Savić Snežana D
1Department of Pharmaceutical Technology and Cosmetology Faculty of Medicine, University of Banja Luka, 78000 Banja Luka Bosnia and Herzegovina.
2Department of Pharmaceutical Technology and Cosmetology Faculty of Pharmacy, University of Belgrade, 11221 Belgrade, Serbia.
Acta Pharm. 2017 Dec 20;67(4):415-439. doi: 10.1515/acph-2017-0036.
Two types of biocompatible surfactants were evaluated for their capability to formulate skin-friendly/non-irritant microemulsions as vehicles for two poorly water-soluble model drugs differing in properties and concentrations: alkyl polyglucosides (decyl glucoside and caprylyl/capryl glucoside) and ethoxylated surfactants (glycereth-7-caprylate/ caprate and polysorbate 80). Phase behavior, structural inversion and microemulsion solubilization potential for sertaconazole nitrate and adapalene were found to be highly dependent on the surfactants structure and HLB value. Performed characterization (polarized light microscopy, pH, electrical conductivity, rheological, FTIR and DSC measurements) indicated a formulation containing glycereth- 7-caprylate/caprate as suitable for incorporation of both drugs, whereas alkyl polyglucoside-based systems did not exhibit satisfying solubilization capacity for sertaconazole nitrate. Further, monitored parameters were strongly affected by sertaconazole nitrate incorporation, while they remained almost unchanged in adapalene-loaded vehicles. In addition, results of the in vivo skin performance study supported acceptable tolerability for all investigated formulations, suggesting selected microemulsions as promising carriers worth exploring further for effective skin delivery of model drugs.
评估了两种生物相容性表面活性剂，以确定它们制备对皮肤友好/无刺激性微乳液的能力，该微乳液作为两种性质和浓度不同的难溶性模型药物的载体：烷基多苷（癸基葡糖苷和辛酰/癸酰葡糖苷）和乙氧基化表面活性剂（甘油聚醚-7-辛酸酯/癸酸酯和聚山梨酯80）。发现硝酸舍他康唑和阿达帕林的相行为、结构转变和微乳液增溶潜力高度依赖于表面活性剂的结构和HLB值。进行的表征（偏光显微镜、pH值、电导率、流变学、傅里叶变换红外光谱和差示扫描量热法测量）表明，含有甘油聚醚-7-辛酸酯/癸酸酯的制剂适合两种药物的掺入，而基于烷基多苷的体系对硝酸舍他康唑没有表现出令人满意的增溶能力。此外，监测参数受硝酸舍他康唑掺入的强烈影响，而在载有阿达帕林的载体中它们几乎保持不变。此外，体内皮肤性能研究结果支持所有研究制剂的可接受耐受性，表明所选微乳液作为有前途的载体，值得进一步探索用于模型药物的有效皮肤递送。
