白杨素脂质体的制备工艺优化及抗神经炎症活性研究  

Preparation optimisation and anti-neuroinflammation activity of liposomes chrysin

作　　者：贾文 丁文华 汪凯康 王丹[2] 徐维平 JIA Wen;DING Wen-hua;WANG Kai-kang;WANG Dan;XU Wei-ping(College of Pharmacy,Anhui University of Chinese Medicine,Hefei 230012;University of Science and Technology of China,Hefei 230027;Anhui Institute of Gerontology,Department of Gerontology,First Affiliated Hospital of University of Science and Technology of China,Hefei 230001)

机构地区：[1]安徽中医药大学药学院,合肥230012 [2]中国科学技术大学,合肥230027 [3]安徽省老年医学研究所,中国科学技术大学附属第一医院老年医学科,合肥230001

出　　处：《中南药学》2024年第4期864-870,共7页Central South Pharmacy

基　　金：国家自然科学基金项目(No.52072360)。

摘　　要：目的 优化白杨素脂质体的制备工艺并研究其体外抗神经炎症活性。方法 采用乙醇注入法制备白杨素脂质体,根据单因素实验结果,通过Box-Behnken响应面筛选最优处方并表征。细胞毒性实验确定白杨素及其脂质体的安全药物浓度范围,利用脂多糖(LPS)诱导的BV2细胞分析白杨素脂质体的抗神经炎症活性。结果 白杨素脂质体最佳制备工艺参数:磷脂与胆固醇比7.86∶1、搅拌速度615 r·min^(-1)、水浴温度60℃,制备的白杨素脂质体形态呈椭圆球形,包封率为(85.01±0.33)%,平均粒径为(141.43±0.5)nm,平均PDI为(0.240±0.021),体外释药具有明显的缓释特征。细胞实验结果显示,在0~100μmol·L^(-1)实验浓度范围内,空白脂质体对BV2细胞无明显的细胞毒性。抗炎性能分析表明,相较于游离白杨素,白杨素脂质体对LPS诱导的BV2细胞具有更强的抗炎效果,且在使用范围(<25μmol·L^(-1))内无细胞毒性。结论 本研究成功制备并优化了白杨素脂质体,该制剂提高了白杨素的溶解度和体外释放性能,同时展现出良好的体外抗炎活性,为未来白杨素新剂型的开发提供了理论基础。Objective To optimize the preparation of chrysin liposomes by response surface methodology and determine their in vitro anti-neuroinflammation activity.Methods The chrysin liposome was prepared by ethanol injection.According to the results of single factor experiment,the optimal prescription was screened and characterized by Box-Behnken response surface.Cytotoxicity experiments determined the safe drug concentration range of chrysin and chrysin liposome,and lipopolysaccharide(LPS)was used to analyze the anti-neuroinflammation activity in BV2 cells.Results Parameters for the optimal preparation of chrysin liposomes were as follows:lipid-cholestero-7.86∶1,stirring at 615 r·min 1,and temperature at 60℃.The morphology of chrysin liposome prepared under this condition was elliptical,with encapsulation rate(85.01±0.33)%,the average particle size(141.43±0.5)nm,and PDI(0.240±0.021).In vitro drug release showed obvious characteristics of sustained release.In vitro cell experiments indicated:the experimental concentration-range of 0~100μmol·L^(-1),blank liposomes without cells cytotoxicity on BV2 microglia.Anti-inflammatory performance indicated that as compared to free chrysin,chrysin liposomes had stronger-anti-inflammatory effecting,and were no cytotoxicity within the range of use(<25μmol·L^(-1)).Conclusion This study successfully prepares and optimizes chrysin liposomes,improves the solubility and release performance of chrysin in vitro,and showes good anti-inflammatory activity in vitro,providing a theoretical basis for the development of new formulations of chrysin.

关 键 词：白杨素 脂质体 响应面法 神经炎症 

分 类 号：R283[医药卫生—中药学] R285[医药卫生—中医学]