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氢化可的松从桉叶油微乳剂的透皮给药:助表面活性剂的影响。

Transdermal delivery of hydrocortisone from eucalyptus oil microemulsion: effects of cosurfactants.

作者信息

El Maghraby Gamal M

机构信息

Department of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh 11451, P.O. Box 2457, Saudi Arabia.

出版信息

Int J Pharm. 2008 May 1;355(1-2):285-92. doi: 10.1016/j.ijpharm.2007.12.022. Epub 2007 Dec 24.

Abstract

This study investigated the effects of cosurfactants on the transdermal delivery of hydrocortisone (model drug) from eucalyptus oil microemulsion. Eucalyptus oil which was successfully employed for steroidal drugs was used as the oil. Tween 80 which was readily miscible with eucalyptus oil was used as surfactant. Ethanol, isopropanol and propylene glycol which are relatively tolerable by the skin were employed as cosurfactants. Pseudo-ternary phase diagrams were constructed in the presence and absence of cosurfactants. Microemulsion formulations containing 20% oil, 20% water and 60% of either Tween 80 or 1:1 surfactant/cosurfactant mixture were compared. Incorporation of cosurfactants expanded the microemulsion zone. The cosurfactant free microemulsion was viscous showing pseudo-plastic flow. The cosurfactant containing preparations were less viscous with Newtonian flow. The drug loading and release rate were increased in the presence of cosurfactants with the release depending on the viscosity. Incorporation of hydrocortisone in microemulsion increased the transdermal flux compared to saturated aqueous solution. The presence of cosurfactants increased the transdermal drug flux compared to the cosurfactant free formulation. Ethanol produced the greatest effect followed by propylene glycol and isopropanol. The presence of cosurfactant and its type can thus affect both the phase behavior and the transdermal delivery potential of microemulsion.

摘要

本研究考察了助表面活性剂对氢化可的松(模型药物)从桉叶油微乳透皮给药的影响。将成功用于甾体类药物的桉叶油用作油相。将易与桉叶油混溶的吐温80用作表面活性剂。将皮肤相对耐受的乙醇、异丙醇和丙二醇用作助表面活性剂。绘制了有无助表面活性剂存在时的拟三元相图。比较了含20%油、20%水和60%吐温80或1:1表面活性剂/助表面活性剂混合物的微乳制剂。加入助表面活性剂扩大了微乳区域。不含助表面活性剂的微乳呈粘性,表现出假塑性流动。含助表面活性剂的制剂粘性较小,呈牛顿流动。在有助表面活性剂存在时,药物载药量和释放速率增加,释放取决于粘度。与饱和水溶液相比,微乳中加入氢化可的松可增加透皮通量。与不含助表面活性剂的制剂相比,助表面活性剂的存在增加了透皮药物通量。乙醇的效果最大,其次是丙二醇和异丙醇。因此,助表面活性剂的存在及其类型可同时影响微乳的相行为和透皮给药潜力。

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