首页|白杨素脂质体的制备工艺优化及抗神经炎症活性研究

白杨素脂质体的制备工艺优化及抗神经炎症活性研究

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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.
Preparation optimisation and anti-neuroinflammation activity of liposomes chrysin
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.

chrysinliposomeresponse surface methodologyneuroinflammation

贾文、丁文华、汪凯康、王丹、徐维平

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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

白杨素 脂质体 响应面法 神经炎症

国家自然科学基金

52072360

2024

中南药学
湖南省药学会

中南药学

CSTPCD
影响因子:0.736
ISSN:1672-2981
年,卷(期):2024.22(4)
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