Temperature-Sensitive Microemulsion Gel: An Effective Topical Delivery System for Simultaneous Delivery of Vitamins C and E
Temperature-Sensitive Microemulsion Gel: An Effective Topical Delivery System for Simultaneous Delivery of Vitamins C and E
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DOI：
10.1208/s12249-008-9172-3
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发表时间：
2009-03-01
影响因子：
3.3
通讯作者：
Gasperlin, Mirjana
中科院分区：
文献类型：
--
作者：
Rozman, Branka;Zvonar, Alenka;Gasperlin, Mirjana
微乳液（ME）——由水、油和表面活性剂组成的纳米结构系统——经常被用来尝试增加皮肤药物输送。这项工作的主要目标是开发温度敏感的微乳液凝胶（称为类凝胶ME），作为一种有效且安全的递送系统，适合同时局部施用亲水性维生素C和亲脂性维生素E。通过改变液体o/w ME（o/w ME）的水含量，形成具有温度敏感流变特性的凝胶状ME。通过旋转流变测量、粘度测量和液滴尺寸测定证实了温度驱动的微观结构变化。释放研究表明，在皮肤温度下，凝胶状 ME 中维生素的释放与 o/w ME 的维生素释放相当，并且比传统用聚合物（o/w ME 卡波姆）增稠的 o/w ME 更快、更完全。根据两种维生素皮肤输送的有效性，发现o/w ME最合适，其次是凝胶状ME和o/w ME卡波姆，这表明维生素释放和皮肤吸收之间没有发现简单的相关性。细胞毒性研究表明，暴露于 ME 后细胞具有良好的活力，并证实所有测试的微乳液均无刺激性。
Microemulsions (ME)-nanostructured systems composed of water, oil, and surfactants-have frequently been used in attempts to increase cutaneous drug delivery. The primary objective addressed in this work has been the development of temperature-sensitive microemulsion gel (called gel-like ME), as an effective and safe delivery system suitable for simultaneous topical application of a hydrophilic vitamin C and a lipophilic vitamin E. By changing water content of liquid o/w ME (o/w ME), a gel-like ME with temperature-sensitive rheological properties was formed. The temperature-driven changes in its microstructure were confirmed by rotational rheometry, viscosity measurements, and droplet size determination. The release studies have shown that the vitamins' release at skin temperature from gel-like ME were comparable to those from o/w ME and were much faster and more complete than from o/w ME conventionally thickened with polymer (o/w ME carbomer). According to effectiveness in skin delivery of both vitamins, o/w ME was found the most appropriate, followed by gel-like ME and by o/w ME carbomer, indicating that no simple correlation between vitamins release and skin absorption could be found. The cytotoxicity studies revealed good cell viability after exposure to ME and confirmed all tested microemulsions as nonirritant.