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目的:研制博莱霉素(BLM)脂质体凝胶,并对其皮肤靶向性进行体外评价。方法:采用逆相蒸发-冻融法制备BLM脂质体,再用卡波姆940为基质制成BLM脂质体凝胶;以离心法测定BLM脂质体的包封率;以体外透皮渗透释药法,比较BLM脂质体凝胶与BLM普通凝胶的透过作用。结果:BLM脂质体平均粒径为(885.20±12.08)nm,平均包封率为(66.80±1.38)%。在24h内,BLM脂质体凝胶累积透过量(Q)及稳态透皮速率(J)与BLM普通脂质体相比,均明显提高,而在皮肤中的滞留药量也显著提高(P<0.05)。结论:BLM脂质体凝胶在体外可显著增加BLM的透皮吸收,增加皮肤中的滞留量,值得进一步研究。
Objective: To develop BLM liposome gel and evaluate its skin targeting in vitro. Methods: BLM liposomes were prepared by reversed-phase evaporation-freeze-thaw method. BLM liposomes gel was made by using carbomer 940 as matrix. The encapsulation efficiency of BLM liposomes was determined by centrifugation. Osmotic release method, compared BLM liposome gel and BLM ordinary gel permeation. Results: The average diameter of BLM liposomes was (885.20 ± 12.08) nm, the average entrapment efficiency was (66.80 ± 1.38)%. Within 24 h, the cumulative permeation volume (Q) and steady-state transdermal rate (BL) of BLM liposomes increased significantly compared with those of BLM liposomes, while the amount of drug retention in the skin was also significantly increased P <0.05). Conclusion: BLM liposome gel in vitro can significantly increase the transdermal absorption of BLM, increase the retention of the skin, deserves further study.