塞来昔布脂质体凝胶的研制及其体外经皮渗透动力学考察

目的研制塞来昔布脂质体凝胶,并对其体外经皮渗透动力学进行考察。方法采用薄膜分散法制备塞来昔布脂质体,均匀设计筛选最佳处方及制备工艺,并以卡波姆940为基质制成脂质体凝胶;用Franz扩散池研究塞来昔布脂质体凝胶与塞来昔布普通凝胶的经皮渗透规律。结果塞来昔布脂质体凝胶的平均粒径为(369.5±10.8)nm,平均包封率为(81.6±2.2)%(n=3);体外透皮试验表明塞来昔布脂质体凝胶的累积透过量显著大于普通凝胶(P<0.05),药物透皮速率与皮肤蓄积量显著大于普通凝胶(P<0.01)。结论塞来昔布脂质体凝胶制备简单,能促进药物透皮吸收,值得进一步研究。

Preparation of celecoxib liposomal gels and its transdermal permeation kinetics in vitro

AIM To prepare celecoxib(CLX) liposome gels and to study its transdermal permeation kinetics in vitro.METHODS The CLX liposomes were prepared by the film dispersion method.The uniform design was used to obtain the optimal formulation and preparation process.Carbopol 940 was used as the gelling agent.The permeation rate of CLX liposomal gels were compared with that of CLX common gels by Franzdiffusion cells in vitro.RESULTS Mean diameter of the CLX liposomes was(369.5±10.8) nm and average entrapment efficiency was(81.6±2.2)%(n=3).The cumulative penetration of the CLX liposomal gels was higher than that of the common gels(P < 0.05),and its transdermal penetration rate and the amount of skin retention were much higher than those of the common gels(P < 0.01).CONCLUSION The CLX liposomal gels is easy to prepare.It can enhance the transdermal permeation of CLX in vitro,and is valuable for further study.