首页|芍药苷聚乳酸-羟基乙酸共聚物纳米粒制备工艺的优化及对心肌细胞的保护作用

芍药苷聚乳酸-羟基乙酸共聚物纳米粒制备工艺的优化及对心肌细胞的保护作用

扫码查看
目的:优化芍药苷聚乳酸-羟基乙酸共聚物(PLGA)纳米粒制备工艺,并探讨芍药苷PLGA纳米粒对H2O2诱导损伤的H9c2心肌细胞的保护作用.方法:首先使用复乳-溶剂挥发法制备芍药苷PLGA纳米粒,采用Plackett-Burman设计实验以及Box-Behnken响应面设计实验对其制备工艺进行优选,得出最佳处方,并对按最佳处方制备的芍药苷PLGA纳米粒进行表征分析、4℃储藏稳定性考察以及体外释放考察;最后通过H2O2诱导建立大鼠H9c2心肌细胞氧化损伤模型,考察芍药苷PLGA纳米粒对心肌细胞的保护作用,CCK-8法检测细胞存活率,试剂盒检测心肌细胞乳酸脱氢酶(LDH)漏出量、丙二醛(MDA)、超氧化物歧化酶(SOD)的含量.结果:最佳处方:泊洛沙姆浓度为0.4%,给药量为3.1 mg,PLGA为21.4 mg;所得芍药苷PLGA纳米粒包封率为(45.49±0.29)%,载药量为(4.52±0.05)%,粒径为(115.1±3.61)nm,多分散系数(polydiseperse index,PDI)为(0.122±0.01),Zeta 电位为-(23.2±0.19)mV,形态为规则圆形,体外释放12 h释放率为80%;细胞实验结果表明芍药苷PLGA纳米粒能提高心肌细胞存活率,降低LDH和MDA含量,升高SOD含量(P<0.05).结论:优化所得芍药苷PLGA纳米粒制备工艺可行,所得纳米粒稳定性好,具有缓释作用,体外释放符合Ritger-Peppas动力学模型;芍药苷PLGA纳米粒对H2O2诱导损伤的H9c2心肌细胞具有明显的保护作用.
Preparation process optimization of paeoniflorin PLGA nanoparticle and its protection of cardiomyocytes
Objective:To optimize the preparation process of paeoniflorin PLGA nanoparticles and to explore the protective effect of paeoniflorin nanoparticles on H2O2-injured H9c2 cardiomyocytes.Methods:Paeoniflorin PLGA nanoparticles were prepared by compound emulsion-solvent volatilization method,and Plackett-Burman design combined with Box-Behnken-response surface design was used to optimize the preparation process to obtain the optimum prescription.The surface features,4 ℃ storage situation and in vitro release of paeoniflorin PLGA nanoparticles prepared according to the best prescription were analyzed.The protective effect of paeoniflorin PLGA nanoparticles on H2O2-injured H9c2 cardiomyocytes was studied.The cell survival rate was measured by CCK-8 method.The amount of lactate dehydrogenase(LDH),malondialdehyde(MDA)and superoxide dismutase(SOD)were detected by commercial kits.Results:The optimized prescription is as follows:Poloxamer concentration 0.4%,paeoniflorin 3.1 mg,PLGA 21.4 mg,obtaining encapsulation efficiency is(45.49±0.29)%,loading efficiency is(4.52±0.05)%,particle size is(115.1±3.61)nm,polydiseperse index(PDI)is(0.122± 0.01),and Zeta potential is-(23.2±0.19)mV.It's regular and round in shape and the in vitro release was 80%in 12 h.The cell experiment results showed that paeoniflorin PLGA nanoparticles improved the survival rate of cardiomyocytes,reduced the LDH and MDA content,and increased the SOD content(P<0.05).Conclusion:The optimized paeoniflorin PLGA nanoparticles were stable at 4 ℃ and released slowly in vitro.The rule of its release fits the Ritger-Peppas kinetic model.Paeoniflorin PLGA nanoparticles showed obvious protection against H2O2-induced damage in H9c2 cardiomyocytes.

paeoniflorinPLGA nanomarticlesPlackett-BurmanBox-Behnken response methodH9c2 cardiomyocytesoxidative damage

肖奕菲、陆慧玲、杜利新、郭志华、李雅

展开 >

湖南中医药大学,长沙 410208

芍药苷 PLGA纳米粒 Plackett-Burman Box-Behnken响应面法 H9c2心肌细胞 氧化损伤

湖南省卫生健康委科研课题湖南中医药大学中药学一流学科建设项目

D2023030178614901-0200002006

2024

中国新药杂志
中国医药科技出版社 中国医药集团总公司 中国药学会

中国新药杂志

CSTPCD北大核心
影响因子:1.039
ISSN:1003-3734
年,卷(期):2024.33(5)
  • 24