尼美舒利脂质体凝胶的研制及体外经皮渗透动力学考察

 目的研制尼美舒利(nimesulide,NIM)脂质体凝胶,并进行体外经皮渗透动力学研究。方法通过均匀实验设计筛选NIM脂质体的最佳处方,采用薄膜分散法制备NIM脂质体,再以泊洛沙姆-407为基质制成脂质体凝胶;以影响因素试验考察该制剂的稳定性,并用Franz扩散池研究NIM脂质体凝胶与NIM凝胶的经皮渗透规律。结果NIM脂质体平均粒径为(856.6±14.3)nm,Zeta电位为(-13.87±5.3)mV,平均包封率为(77.7±1.4)%(n=3);室温下,NIM脂质体凝胶为黄色细腻黏稠胶体,对湿度及室温条件稳定,但对光照和40℃与60℃不稳定;体外透皮试验表明,NIM脂质体凝胶的累积透过量显著大于NIM凝胶(P<0.05),药物透皮速率与皮肤蓄积量非常显著地大于NIM凝胶(P<0.01)。结论NIM脂质体凝胶制备工艺可行,质量稳定,检测方法可靠,能促进药物透皮渗透,值得进一步研究。

Study on Preparation of Nimesulide Liposome Gel and Its Cutaneous Permeation Kinetics in Vitro

OBJECTIVE To prepare NIM liposomal gel and to study its cutaneous permeation kinetics in vitro.METHODS The uniform design was used to screen the optimal formation and preparation process.The NIM liposome was prepared by the film dispersion method,and the poloxamer407 was added as the base for the preparation of the liposomal gel,The Franzdiffusion cell was employed to compare the permeation rate of NIM liposomal gel with NIM gel in vitro.RESULTS Mean diameter of the NIM liposomes was(856.6±14.3) nm with Zeta-potential of(-13.87±5.3) mV and mean entrapment efficiency of(77.7±1.4)%(n=3).The liposomal gel had a promissing appearance.It was stable to the humidity and the room temperature while was sensitive to the light and the temperature from 40 ℃ to 60 ℃.The cumulative penetration of NIM liposomal gel was higher than the NIM gel(P<0.05).Its cutaneous penetration rate and cumulative amounts in skin were much higher than those of the NIM gel(P<0.01).CONCLUSION The results suggested that the NIM liposomal gel was valuable to be studied further.