title: Optimization of madecassoside liposomes using response surface methodology and evaluation of its stability.
abstract: 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.
authors.affiliation: School of Chemistry and Chemical Engineering, Guangdong Provincial Key Lab for Green Chemical Product Technology, South China University of Technology, Guangzhou 510640, China.
authors.forename: Huijuan
authors.initials: H
authors.lastname: Wang
authors.affiliation: School of Chemistry and Chemical Engineering, Guangdong Provincial Key Lab for Green Chemical Product Technology, South China University of Technology, Guangzhou 510640, China. Electronic address: liumf@scut.edu.cn.
authors.forename: Meifeng
authors.initials: M
authors.lastname: Liu
authors.affiliation: Guangzhou Hairui Pharmaceutical Co., Ltd. Yangtze River Pharmaceutical Group, Guangzhou 510663, China.
authors.forename: Song
authors.initials: S
authors.lastname: Du
mesh_terms: D002626:Chemistry, Pharmaceutical; D002784:Cholesterol / Q000737:chemistry; D004355:Drug Stability; D054709:Lecithins / Q000737:chemistry; D008081:Liposomes; D008855:Microscopy, Electron, Scanning; D010316:Particle Size; D010710:Phosphates / Q000737:chemistry; D013499:Surface Properties; D014315:Triterpenes / Q000737:chemistry*; D014810:Vitamin E / Q000737:chemistry
chemical_list: D054709:Lecithins; D008081:Liposomes; D010710:Phosphates; D014315:Triterpenes; D014810:Vitamin E; D002784:Cholesterol; C093443:madecassoside; C018279:sodium phosphate
keywords: Encapsulation efficiency; Madecassoside (MA) liposomes; Physical stability; Response surface methodology (RSM)