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
贾文 1丁文华 1汪凯康 1王丹 2徐维平3
作者信息
- 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. 安徽中医药大学药学院,合肥 230012;中国科学技术大学,合肥 230027;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
- 折叠
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615r·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0～100 μmol·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.
Abstract
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 0～100 μmol·L-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(＜25 μmol·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Key words
chrysin/liposome/response surface methodology/neuroinflammation引用本文复制引用
出版年
2024
NETL
NSTL
万方数据