Wang Huijuan, Liu Meifeng, Du Song
School of Chemistry and Chemical Engineering, Guangdong Provincial Key Lab for Green Chemical Product Technology, South China University of Technology, Guangzhou 510640, China.
School of Chemistry and Chemical Engineering, Guangdong Provincial Key Lab for Green Chemical Product Technology, South China University of Technology, Guangzhou 510640, China.
Int J Pharm. 2014 Oct 1;473(1-2):280-5. doi: 10.1016/j.ijpharm.2014.07.010. Epub 2014 Jul 8.
Polar compounds with large molecular weight have poor membrane permeability, liposomes can promote drugs to penetrate epidermis and remain or release at dermis. Madecassoside (MA) exhibits powerful potency in treatment of skin disorders such as wound healing, scar management, and psoriasis, but it is not easy to penetrate epidermis for its hydrophilic nature. The aim of this work is to get the optimum process conditions and evaluate physicochemical properties and physical stability of MA liposomes. In order to avoid this disadvantage and maintain long term drug storage, MA Liposomes were designed to achieve optimum preparation conditions using response surface methodology (RSM) in our experiment. The process and formulation variables were optimized by achieving maximum drug encapsulation efficiency. The optimum conditions were 0.4424 g of madecassoside, 8.174 of ratio of egg yolk lecithin to cholesterol, 65 s of ultrasonic time. The results of particle size, zeta potential and encapsulation efficiency of madecassoside liposomes were 293 nm, -35.6 mV, and 40.90%, respectively, on the basis of the above optimum conditions. According to the morphology of liposomes and encapsulation efficiency of triplicate experiments conducted at optimum conditions, MA liposomes obtained by this optimized formulation had characters of favorable repeatability and proper particle size. The physical stability tests of MA liposomes indicated that its suitable storage temperature was at 4°C with higher encapsulation efficiency.
大分子极性化合物的膜通透性较差，脂质体可促进药物穿透表皮并在真皮层滞留或释放。积雪草苷（MA）在治疗伤口愈合、瘢痕管理和银屑病等皮肤疾病方面具有强大功效，但因其亲水性，不易穿透表皮。本研究的目的是获得最佳工艺条件，并评估MA脂质体的理化性质和物理稳定性。为避免这一缺点并保持药物长期储存，在我们的实验中，采用响应面法（RSM）设计MA脂质体以实现最佳制备条件。通过实现最大药物包封率来优化工艺和配方变量。最佳条件为积雪草苷0.4424 g、蛋黄卵磷脂与胆固醇比例8.174、超声时间65 s。基于上述最佳条件，积雪草苷脂质体的粒径、ζ电位和包封率结果分别为293 nm、-35.6 mV和40.90%。根据在最佳条件下进行的三次重复实验的脂质体形态和包封率，通过这种优化配方获得的MA脂质体具有良好的重复性和合适的粒径。MA脂质体的物理稳定性测试表明，其适宜的储存温度为4°C，包封率较高。
