积雪草苷柔性纳米脂质体凝胶剂的研制及体外评价

Preparation and in vitro Evaluation of Asiaticoside Ultraflexible Liposomal Gel

采用乙醇注入-高压均质法制备积雪草苷柔性纳米脂质体,所得制品平均粒径为(76.20±2.80)nm,多分散性系数为(0.10±0.02),电位为(-41.40±3.20)mV,包封率为(91.94±2.56)%。再将其制成以甲基纤维素为凝胶基质的凝胶剂,并以普通凝胶剂为对照考察了两种剂型中积雪草苷对离体小鼠皮肤的体外透皮情况。结果表明,两种剂型中积雪草苷的经皮稳态渗透速率分别为16.15和3.34 g·cm-2·h-1,皮内滞留量分别为(14.99±0.58)和(6.76±0.39)g/cm2。

The asiaticoside ultraflexible liposomes were prepared by ethanol injection method with high pressure homogenization. The nanometer-sized particles with the mean diameter of （76.20±2.80）nm and polydispersity index of （0.10±0.02） were obtained. The ζ potential and entrapment efficiency of the product were （-41.40±3.20）mV and （91.94±2.56） %, respectively. The asiaticoside ultraflexible liposomal gel with methylcellulose as the gel matrix was prepared by adding above liposomes into the gel matrix. The in vitro transdermal delivery of asiaticoside from the prepared liposomal gel and common gel through the excised mouse skin were investigated. The results showed that the average steady-state fluxes of asiaticoside from the liposomal gel and common gel were 16.15 and 3.34 μg.cm-2.h-1, respectively. The skin retention of above preparations were （14.99±0.58） and （6.76±0.39） μg/cm2, respectively.