Mao Yan-Ting, Hua Hai-Ying, Zhang Xiang-Guo, Zhu Dong-Xue, Li Feng, Gui Zhen-Hua, Zhao Yong-Xing
School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou, Henan, PR China.
Pharmazie. 2013 May;68(5):381-2.
The purpose of the present study was to develop a novel transdermal vinpocetine patch containing a stable formulation and with good entrapment efficiency, and percutaneous absorption which via ethosome. Ethosome was found to be a more efficient delivery carrier with high encapsulation capacities (79.5% +/- 1.8%) and nanometric size (180.7 +/- 1.5 nm). In vitro percutaneous permeation experiments demonstrated that the permeation of vinpocetine through abdominal skin of Sprague Dawley was significantly increased when ethosome was used. The vinpocetine transdermal fluxes from ethosome gel (3.56 +/- 0.13 microg/cm2/h) were 6.72 and 3.10 times higher than that of vinpocetine gel solution and vinpocetine aueous solution, respectively. Furthermore, the AUC(0 --> infinity), and eliminiation half-life by the transdermal administration were significantly higher than those by the intragastric administration (P < 0.01). The study demonstrated that ethosome is a promising vesicular carrier for enhancing percutaneous absorption of vinpocetine.
本研究的目的是开发一种新型的含有稳定制剂、具有良好包封率以及通过醇质体实现经皮吸收的长春西汀透皮贴剂。醇质体被发现是一种更高效的递送载体，具有高包封能力（79.5%±1.8%）和纳米尺寸（180.7±1.5nm）。体外经皮渗透实验表明，当使用醇质体时，长春西汀透过Sprague Dawley大鼠腹部皮肤的渗透显著增加。来自醇质体凝胶的长春西汀经皮通量（3.56±0.13μg/cm²/h）分别比长春西汀凝胶溶液和长春西汀水溶液高6.72倍和3.10倍。此外，经皮给药的AUC(0→∞)和消除半衰期显著高于胃内给药（P<0.01）。该研究表明，醇质体是一种有前景的囊泡载体，可增强长春西汀的经皮吸收。
