脂质体影响荧光素钠透皮和皮肤贮留量的实验研究

Effect of liposome on permeability and drug retention of sodium fluorescein in human skin:an experimental study

目的:观察脂质体包裹荧光素钠对人皮肤透皮性能和在皮肤分布的影响。方法:采用Franz扩散池、荧光显微镜和荧光分光光度计研究真、表皮中荧光素钠的分布和含量。结果:荧光素钠脂质体同其溶液和乳剂比较,在表皮内荧光分布深,在真皮荧光强度小;脂质体荧光素钠真皮透过量少,各时间点表皮内荧光含量较溶液剂型高,而真皮内荧光含量较乳剂低,不同剂型各时间点的差异均具有统计学意义(P<0.05)。结论:皮肤外用制剂中脂质体包裹水溶性药物可在人皮肤表皮层保持较高浓度,真皮贮留量和累积透皮量小,故适用于病变表浅的皮肤病,以及经透皮吸收后有不良反应的药物。

Objective： To investigate the effect of liposome on the permeability and drug distribution of sodium fluorescein （NaF1） in human skin. Methods： With an improved Franz diffusion cell and 0.125% NaF1 liposome suspension as the model drug, the distribution of fluorescence in human skin was observed under fluorescence microscope at 4, 8 and 12 h respectively after the diffusion experiment had started. NaFI solution and NaFI emulsion of the same concentration as the model drugs served as the control for this experiment. With a spectrofluorometer, the content of fluorescence in different lays of skin was observed at 4, 8, 12, 24 h respectively. Results： In comparison with NaFI solution and NaF1 emulsion, liposomal NaFI suspension resulted in higher fluorescence intensity in human epidermis and lower fluorescence intensity in the dermis. Conclusions： Local high drug concentrations can be achieved in the epidermis by liposomal suspension of water soluble drug for more effective treatment of epidermal diseases.