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目的:研制吡喹酮(PQ)的脂质体凝胶(PQ-LG),并对其体外释药特性进行考察。方法:薄膜分散法制备PQ脂质体,以泊洛沙姆-407为凝胶基质,研制PQ-LG。采用均匀设计对PQ-LG的处方及制备工艺进行优化,对其体外主要性质进行考察,并采用鼠皮为吸收屏障,对其体外透皮透皮速度及程度进行评价。结果:PQ-LG的最佳处方及工艺条件为:类脂/药物为20∶1,pH为6.5,蒸发温度为45℃,水化时间为30 min。体外性质表明PQ-LG外形圆整,平均粒径为(866.6±18.8)nm,平均包封率(ER)为74.33±1.95%(n=3);体外透皮实验表明PQ-LG的透皮累积透过量Q符合Higuchi方程:Q=34.15t_(1/2)-22.76(r=0.994 8),与PQ凝胶相比,Q及稳态透皮速率J均有明显提高(P<0.05)。结论:PQ-LG具有制备简单,质量理想,透皮吸收好等特点,值得进一步进行体内研究。
Objective: To develop PQ-liposome gel (PQ-LG) and study its in vitro release characteristics. Methods: PQ liposomes were prepared by membrane dispersion method. PQ-LG was prepared by using poloxamer-407 as gel matrix. The uniform design was used to optimize the formulation and preparation of PQ-LG. The main properties of PQ-LG in vitro were investigated. The rat skin was taken as the absorption barrier to evaluate the transdermal skin penetration rate and extent. Results: The optimum prescription and technological conditions of PQ-LG were: lipid / drug 20: 1, pH 6.5, evaporation temperature 45 ℃, and hydration time 30 min. The in vitro properties of PQ-LG showed that the shape of PQ-LG was round and the average particle size was (866.6 ± 18.8) nm with an average entrapment efficiency (ER) of 74.33 ± 1.95% (n = 3) The cumulative permeation Q was in accordance with Higuchi’s equation: Q = 34.15t 1/2 (-22.76) (r = 0.994 8). Compared with PQ gel, Q and steady-state transdermal rate J were significantly increased . Conclusion: PQ-LG has the characteristics of simple preparation, ideal quality and good transdermal absorption, so it is worth further study in vivo.