异甘草素聚乳酸纳米粒的制备及在大鼠体内药动学  

Preparation and Pharmacokinetics of Isoliquiritigenin Polylactic Acid Nanoparticles in Rats

作　　者：高青 马记平 GAO Qing;MA Jiping(Department of Medicine,Zhengzhou Shuqing Medical College,Zhengzhou 450064,China)

机构地区：[1]郑州澍青医学高等专科学校基础医学部

出　　处：《医药导报》2020年第1期85-89,共5页Herald of Medicine

基　　金：河南省教育厅重点项目(16A350006)

摘　　要：目的制备异甘草素聚乳酸纳米粒,考察其在大鼠体内吸收生物利用度。方法采用改良的自乳化溶剂挥发法制备异甘草素聚乳酸纳米粒。激光粒度分析仪测定平均粒径及分布、Zeta电位,并对其包封率、载药量和体外释放情况进行考察。比较异甘草素原料药和异甘草素聚乳酸纳米粒药动学行为及经大鼠灌胃后的吸收生物利用度。结果异甘草素聚乳酸纳米粒平均粒径为(190.22±3.09)nm,多分散性指数(PDI)为0.149±0.039,Zeta电位为(-12.5±0.27)mV,包封率为(74.94±1.18)%,载药量为(8.45±0.66)%。异甘草素聚乳酸纳米粒在体外具有缓慢释药特征,释药过程符合Weibull模型:LnLn[1/(1-M t/M∞)]=0.5194 Lnt-1.3919(r=0.9728)。大鼠体内药动学显示,异甘草素聚乳酸纳米粒的相对生物利用度提高至170.02%。结论异甘草素聚乳酸纳米粒体外具有明显的缓释特征,口服后可有效促进异甘草素体内吸收。Objective To prepare nanoparticles of isoliquiritigenin polylactic acid,and study the effects on the bioavailability of isoliquiritigenin in rats.Methods Isoliquiritigenin polylactic acid nanoparticles were prepared by self-emulsifying solvent volatilization method.The particle size and Zeta potential were determined by laser particle size analyzer.The encapsulation efficiency,drug loading and drug release in vitro of isoliquiritigenin polylactic acid nanoparticles were also studied.The pharmacokinetics and bioavailability of isoliquiritigenin polylactic acid nanoparticles and isoliquiritigenin aqueous suspension after oral administration in rats were studied.Results The particle size,PDI,Zeta potential,encapsulation efficiency and drug loading of isoliquiritigenin polylactic acid nanoparticles were(190.22±3.09)nm,0.149±0.039,(-12.5±0.27)mV,(74.94±1.18)%and(8.45±0.66)%,respectively.The in vivo dissolution experiments showed that isoliquiritigenin polylactic acid nanoparticles had obvious sustained release characterization,the drug release model accord with Weibull model:LnLn[1/(1-M t/M∞)]=0.5194Lnt-1.3919(r=0.9728).The in vivo results of pharmacokinetics in rat model indicated that the relative bioavailability of polylactic acid nanoparticles was enhanced to 170.02%compared with isoliquiritigenin suspension.Conclusion The prepared isoliquiritigenin polylactic acid nanoparticles had obvious sustained release characterization in vitro.After oral administration,it could facilitate the absorption of isoliquiritigenin.

关 键 词：异甘草素 聚乳酸纳米粒 药动学行为 生物利用度 

分 类 号：R979.1[医药卫生—药品] TQ460.6[医药卫生—药学]