Department of Pharmaceutics, School of Pharmaceutical Sciences, Peking University, Beijing 100191, China.
Biomed Res Int. 2013;2013:161943. doi: 10.1155/2013/161943. Epub 2013 Aug 24.
The purpose of this work was to explore the feasibility of ethosomes for improving the antiarthritic efficacy of tetrandrine by topical application. It was found that tetrandrine was a weak base (pK(a) = 7.06) with pH-dependent partition coefficient. The spherical-shaped ethosomes were prepared by pH gradient loading method. Ex vivo permeation and deposition behavior demonstrated that the drug flux across rat skin and deposition of the drug in rat skin for ethosomes was 2.1- and 1.7-fold higher than that of liposomes, respectively. Confocal laser scanning microscopy confirmed that ethosomes could enhance the topical delivery of the drug in terms of depth and quantity compared with liposomes. The ethosomes were shown to generate substantial enhancement of therapeutic efficacy of tetrandrine on Freund's complete adjuvant-induced arthritis with regard to liposomes. These results indicated that ethosomes would be a promising carrier for topical delivery of tetrandrine into and across the skin.
本工作旨在探讨醇质体经皮给药提高汉防己甲素抗关节炎疗效的可行性。研究发现汉防己甲素为弱碱（pK(a) = 7.06），其分配系数具有 pH 依赖性。采用 pH 梯度加载法制备了球形醇质体。离体渗透和沉积行为表明，醇质体的药物经皮通量和药物在大鼠皮肤中的沉积量分别是脂质体的 2.1 倍和 1.7 倍。激光共聚焦扫描显微镜证实，与脂质体相比，醇质体能够增加药物在深度和数量方面的透皮传递。与脂质体相比，醇质体在弗氏完全佐剂诱导的关节炎方面显著提高了汉防己甲素的治疗效果。这些结果表明，醇质体有望成为汉防己甲素经皮递送至皮肤内部和穿过皮肤的一种有前途的载体。
