脂质体影响荧光素钠透皮和皮肤贮留量的实验研究

目的观察脂质体包裹荧光素钠对其透皮和皮肤贮留量的影响。方法选用离体大鼠皮肤进行透皮实验,以0.125%荧光素钠脂质体混悬液为模型药剂,相同浓度的溶液剂作为对照。采用Franz扩散法,用荧光分光光度法检测透皮12 h后扩散池中荧光素钠累积浓度和透皮4 h后皮肤中荧光素钠的贮留量,并在荧光显微镜下观察扩散4 h时皮肤的荧光分布。结果荧光素钠脂质体混悬液同其溶液剂比较,在皮肤内的滞留量大,透皮率低,皮肤荧光强,尤以毛发周围显著。结论皮肤外用制剂中脂质体包裹水溶性药物可在皮肤局部形成较高浓度,有利于皮肤病的治疗。

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

Objective To investigate the effect of liposome on the permeability and drug retention of sodium fluorescein(NaFl) in rat skin. Methods With an improved Franz diffusion cell and 0.125% NaFl liposome suspension as the model drug, in vitro measurement of percutaneous absorption and skin reservoir capacity for NaF1 was conducted using a fluorescence spectrophotometry at 4 and 12 h respectively after the diffusion experiment had started, and distribution of the fluorescence in rat skin was observed under fluorescence microscope at 4 h penetration experiment. NaFl solution of the same concentration as the model drugs served as the control for this experiment. Results In comparison with NaFl solution, liposomal NaFl suspension resulted in larger amount of NaFl retention in rat skin but smaller amount in the receiver cell in a four-hour Franz diffusion test, with also higher fluorescence intensity in the skin, especially the skin around the hair follicles. Conclusion Local high drug concentrations can be achieved in the skin by liposomal suspension of water soluble drug for more effective treatment of skin diseases.