5-氟尿嘧啶脂质体凝胶剂的制备和评价

Preparation and evaluation of 5-Fu Liposomal gel

目的研制5-氟尿嘧啶(5-Fu)脂质体凝胶剂,并进行质量评价。方法采用逆相蒸发-冻融法制备5-Fu脂质体,再用卡波普为基质制成凝胶剂;以离心法测定脂质体的包封率;以体外经皮渗透释药法,比较5-Fu脂质体凝胶剂及5-Fu普通凝胶剂中的经皮渗透作用。结果5-Fu脂质体平均粒径为2.16±0.30μm,平均包封率为(56.17±2.52)%;体外透皮实验中,脂质体凝胶剂24h的药物浓度为158.6mg.mL-1,明显高于普通凝胶剂91.2mg.mL-1。结论载药脂质体凝胶剂可显著减少药物经皮吸收,可维持较长释药时间。

OBJECTIVE To prepare a liposomal gel of 5-Fu and to evaluate it. METHODS The 5-Fu liposome was prepared by the reverse - phase evaporation and freeze - thawing method, the carbopol was added as a support base for the prepartion of the liposomal gel . Encapsulation efficiency was determined by centrifugation ;The permeation rate of 5-Fu liposomal gel was assessed by Franz- diffiusion, and compared with conventional gel. RESULTS Mean diameter of the 5-Fu liposomal was 2.16 ± 0. 30μm and mean encapsulation efficiency was 56. 17 ±2.52% ; The permeation rate of liposomal gel 158.6mg · mL^-1 was significantly higher than that of conventional gel 91.2 mg· mL^-1 in 24h . CONCLUSION Liposomal gel has reduced 5-Fu transcutancous permeation significantly, it can prolong the function duration.