The effect of liposome encapsulation on the percutaneous absorption of norfloxacin through rat skin were examined in vitro and in vivo. In the in vitro transdermal perfusion studies of norfloxacin loaded-liposomes, lipsomal norfloxacin would increase the loading of the drug in stratum corneum. Moreover, the drainage of liposomes from the stratum corneum was somewhat slower than the drug solution from. The increase in the drug retention or stratum corneum for the lipids conformed to the following order: DSPC>DPPC>DMPC. In the in vivo studies, a good correlation was observed between the AUC0-8 in vivo and the flux for permeation experimens in vitro.However, topical applications of liposomal preparations of norfloxacin result in higher and long-lasting amount of drug in the rat skin as compare to oral administration or norfloxacin solution.The liposomal formulations show great potential as a topical drug delivery system. 本研究主要是經由大白鼠之體外與體內實驗,探討微脂粒包覆對norfloxacin經皮吸收的影響。由體外實驗的結果發現,norfloxacin採用微脂粒包覆後可增加藥物在角質層的負載量;同時,微脂粒藥物自角質層的排除速率亦較游離型的藥物緩慢,而組成微脂粒的磷脂層中對藥物在角質層內滯留能力的大小依序是DSPC>DPPC>DMPC。體內實驗八小時所得到的藥物血中濃度曲線下面積,與體外實驗之皮膚通透量間,存在著良好的相關性;而局部使用norfloxacin微脂粒製劑與口服藥物水溶液比較之下,微脂粒包覆藥物在大白鼠皮可產生較高且持續的藥物含量,因此,微脂粒處方在作為局部藥物輸移系統上展現了極大之潛力。