Dragicevic-Curic Nina, Scheglmann Dietrich, Albrecht Volker, Fahr Alfred
Department of Pharmaceutical Technology, Friedrich Schiller University Jena, Lessingstrasse 8, 07743 Jena, Germany.
J Control Release. 2008 Apr 7;127(1):59-69. doi: 10.1016/j.jconrel.2007.12.013. Epub 2007 Dec 26.
Temoporfin (mTHPC) is a highly hydrophobic second generation photosensitizer with low percutaneous penetration. In order to enhance its percutaneous penetration it was necessary to develop a mTHPC-loaded drug carrier system for enhanced skin delivery. mTHPC-loaded invasomes were developed, characterized and investigated for the in vitro percutaneous penetration of mTHPC into abdominal human skin using Franz diffusion cells. mTHPC-loaded invasomes were prepared using non-hydrogenated soybean lecithin (10% w/v), ethanol (3.3% w/v) and a mixture of terpenes (0.5 and 1% w/v). The invasomes obtained were of a sufficiently small particle size (<150 nm) and polydispersity index (<0.3). The particle size of invasomes increased following an increase in the amount of terpenes in the invasomes. All invasomes possessed a negative surface charge. The vesicles appeared to be unilamellar and oligolamellar, spherical and oval in shape. An interesting phenomenon was the finding that with increasing the amount of terpenes, the number of deformed vesicles in the dispersion increased. In vitro skin penetration data revealed that the invasome dispersion with 1% of the mixture of terpenes showed a significantly enhanced deposition (p<0.05) of the drug in the SC compared to liposomes without terpenes and the ethanolic solution.
替莫泊芬（mTHPC）是一种高度疏水的第二代光敏剂，经皮渗透率低。为了提高其经皮渗透率，有必要开发一种用于增强皮肤给药的载mTHPC药物载体系统。制备了载mTHPC的侵入体，对其进行了表征，并使用Franz扩散池研究了mTHPC在体外经皮渗透进入人腹部皮肤的情况。载mTHPC的侵入体采用非氢化大豆卵磷脂（10% w/v）、乙醇（3.3% w/v）和萜烯混合物（0.5%和1% w/v）制备。所得侵入体粒径足够小（<150 nm），多分散指数<0.3。随着侵入体中萜烯含量的增加，侵入体的粒径增大。所有侵入体均带负表面电荷。囊泡似乎是单层和多层的，形状为球形和椭圆形。一个有趣现象是发现随着萜烯含量增加，分散体中变形囊泡的数量增加。体外皮肤渗透数据显示，与不含萜烯的脂质体和乙醇溶液相比，含1%萜烯混合物的侵入体分散体在角质层中的药物沉积显著增强（p<0.05）。
