Fang J Y, Sung K C, Lin H H, Fang C L
Graduate Institute of Pharmaceutical Sciences, Taipei Medical College, 250 Wu-Hsing Street, Taipei, Taiwan.
J Control Release. 1999 Jun 28;60(1):1-10. doi: 10.1016/s0168-3659(99)00055-3.
The major purpose of this work was to study the effect of various liposome formulations on the iontophoretic transport of enoxacin through excised rat skin. The electrochemical stability of these liposomes was also evaluated. The encapsulation percentage of enoxacin was significantly enhanced after 6 h incubation in an electric field; whereas the fusion of liposomes was inhibited by application of electric current. The results of iontophoretic drug transport showed that the permeability of enoxacin released from liposomes was higher compared with that of free drug. The iontophoretic permeability of enoxacin released from liposomes increased with a decrease in the fatty acid chain length of the phospholipid, which may be due to the different phase transition temperatures of the phospholipids. Incorporation of charged phospholipid resulted in an alteration of the transdermal behavior of enoxacin: the iontophoretic permeation as well as the amount of enoxacin partitioned in skin was greatly reduced after incorporation of stearylamine in liposomes, which can be attributed to the competitive ion effect. The enoxacin released from stratum corneum-based liposomes showed the highest amount of enoxacin partitioned into skin depot. The results of employing cathodal iontophoresis on negative charged liposomes suggested that the liposomal vesicles or phospholipids may carry enoxacin into deeper skin strata via the follicular route.
这项工作的主要目的是研究各种脂质体制剂对依诺沙星经离体大鼠皮肤离子导入转运的影响。还评估了这些脂质体的电化学稳定性。在电场中孵育6小时后,依诺沙星的包封率显著提高;而电流的施加抑制了脂质体的融合。离子导入药物转运结果表明,与游离药物相比,脂质体释放的依诺沙星的渗透性更高。脂质体释放的依诺沙星的离子导入渗透性随磷脂脂肪酸链长度的缩短而增加,这可能是由于磷脂的不同相变温度所致。加入带电磷脂会导致依诺沙星透皮行为的改变:在脂质体中加入硬脂胺后,离子导入渗透以及依诺沙星在皮肤中的分配量大大降低,这可归因于竞争离子效应。从基于角质层的脂质体释放的依诺沙星在皮肤贮库中的分配量最高。对带负电荷脂质体采用阴极离子导入的结果表明,脂质体囊泡或磷脂可能通过毛囊途径将依诺沙星携带到更深的皮肤层。
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