Temoporfin-loaded invasomes: Development, characterization and in vitro skin penetration studies
Temoporfin-loaded invasomes: Development, characterization and in vitro skin penetration studies
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DOI：
10.1016/j.jconrel.2007.12.013
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发表时间：
2008-04-07
影响因子：
10.8
通讯作者：
Fahr, Alfred
中科院分区：
文献类型：
--
作者：
Dragicevic-Curic, Nina;Scheglmann, Dietrich;Fahr, Alfred
替莫普芬(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mTHPC的透皮吸收能力，有必要研制一种mTHPC载药系统，以增强其经皮给药。利用Franz扩散池，研究了mTHPC的体外透皮吸收特性，建立了mTHPC的侵入体。以非氢化大豆卵磷脂(10%w/v)、乙醇(3.3%w/v)和萜烯混合物(0.5%和1%w/v)制备mTHPC载体。得到的侵染体具有足够小的颗粒尺寸(~lt；150 nm)和多分散指数(~lt；0.3)。随着侵染体中萜类化合物含量的增加，侵染体的颗粒也随之增大。所有的侵入体表面都带负电荷。囊泡呈单层和少层，球形、椭圆形。一个有趣的现象是，随着萜烯含量的增加，分散体中变形的囊泡数量增加。体外透皮实验表明，含1%混合萜类化合物的侵袭体分散体显著促进了药物的沉积(P<0.05)。
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