积雪苷柔性纳米脂质体的制备与表征分析

Analysis on preparation and characterization of asiaticosideloaded flexible nanoliposomes

积雪苷是中药积雪草的有效成分,临床主要用于促进手术创面愈合和瘢痕修复,治疗效果明显。然而其透皮吸收差和作用时间短限制了药物的推广应用。本实验采用逆相-挤出-冻干法制备积雪苷柔性脂质体冻干制剂,测定了其电镜结构、粒径、Zeta电位、包封率、载药量、稳定性和药物释放特征,并采用智能透皮吸收仪测定柔性脂质体膏体的体外透皮作用。积雪苷柔性脂质体为白色球状,pH 7.03,粒径70.14 nm,Zeta电位-36.5 mV,3批样品的平均包封率为31.43%,3批冻干样品每1 mg含积雪苷的平均值为0.134 mg,显示积雪苷柔性脂质体具有良好的理化性质和药学特征,并且提高了药物的透皮性能。

Asiaticoside is a compound extracted from traditional Chinese medicine Centella asiatica, and mainly used in wound healing and scar repair in clinical, with notable efficacy. However, its poor transdermal absorption and short action time restrict its wide application. In this experiment, the reserve-phase-extrusion-lyophilization method was conducted to prepare the lyophilized asiati- coside-loaded flexible nanoliposomes （LAFL）. Its characteristics including electron microscope structure, particle size, Zeta potential, entrapment rate, drug-loading rate, stability and drug release were determined with the intelligent transdermal absorption instrument. LAFL were white spheroids, with pH, particle size and zeta potential of 7. 03, 70. 14 nm and - 36. 5 mV, respectively. The average entrapment rate of the 3 batch samples were 31.43%, and the average asiaticoside content in 1 mg lyophilized simple was O. 134 mg. The results indicated that LAFL have good physicochemical properties and pharmaceutical characteristics, with an improved transdermal performance.