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白藜芦醇纳米混悬剂的制备及体外初步评价

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目的 制备白藜芦醇(RES)纳米混悬剂,并进行体外评价.方法 采用沉淀法制备RES纳米混悬剂.以平均粒径及多分散系数(PDI)为评价指标,正交试验优化制剂工艺.冷冻干燥法制备纳米混悬剂冻干粉末并进行表征.使用透析袋法研究制剂的体外释放情况.建立高糖刺激的ARPE-19细胞损伤模型,CCK-8法评估RES纳米混悬剂对细胞活力的影响.结果 RES最优处方工艺为:RES浓度6 mg/mL,两种稳定剂(PVP K17∶HPMC)质量比2∶1,RES与稳定剂质量比1∶2,5%甘露醇做冻干保护剂.RES纳米混悬剂为相对规则的颗粒状,载药量为28.04%,36 h内累计释放量达91.27%.与RES相比,RES纳米混悬剂预处理后ARPE-19细胞活力显著提高(P<0.05).结论 RES纳米混悬剂可提高RES的体外释放率,并且能够减轻高糖对ARPE-19细胞的损伤,提高细胞存活率.
Preparation and preliminary evaluation in vitro of resveratrol nanosuspensions
Objective To prepare and in vitro evaluate the resveratrol(RES)nanosuspension.Methods RES nanosuspensions were prepared by precipitation method.With the average particle size and the polydispersity index(PDI)as evaluation indexes,the orthogonal test was used to optimize the formulation process.The freeze-dried powder of nanosuspension was prepared by freeze-drying method and characterized.The in vitro release of the preparation was studied by dialysis bag method.The ARPE-19 cell injury model was estab-lished by high glucose stimulation,and the effect of RES nanosuspension on the cell viability was evaluated by CCK-8 method.Results The optimal prescription process of RES was as follows:the concentration of RES was 6 mg/mL,the mass ratio of two stabilizers(PVP K17∶HPMC)was 2∶1,and the mass ratio of RES and stabilizer was 1∶2,and 5%mannitol was freeze-dried protective agent.The RES nanosuspension was relatively regular granule,with a drug loading of 28.04%and a cumulative release of 91.27%within 36 h.Compared with RES,RES nanosuspension pretreatment significantly increased the viability of ARPE-19 cells damaged by high glucose.Conclusion RES nanosuspension could increase the release rate of RES in vitro,and could attenuate the damage of ARPE-19 cells by high glucose and improve the cell survival rate.

resveratrolnanosuspensionARPE-19 cellshigh glucose-induced cell damagein vitro cumulative release rate

李梦婷、褚琳、何宁、刘家佳、徐维平

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安徽中医药大学药学院,合肥 230012

中国科学技术大学附属第一医院,安徽省立医院眼科

中国科学技术大学附属第一医院,安徽省立医院药剂科

安徽省老年医学研究所,中国科学技术大学附属第一医院,安徽省立医院老年医学科

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白藜芦醇 纳米混悬剂 ARPE-19细胞 高糖致细胞损伤 体外累计释放率

国家自然科学基金项目

52072360

2024

山西医科大学学报
山西医科大学

山西医科大学学报

CSTPCD
影响因子:0.931
ISSN:1007-6611
年,卷(期):2024.55(7)
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