阿苯达唑聚氰基丙烯酸正丁酯纳米粒的制备、性质及其组织靶向性研究阿苯达唑聚氰基丙烯酸正丁酯纳米粒的制备、性质及其组织靶向性研究

目的制备阿苯达唑聚氰基丙烯酸正丁酯纳米粒（albendazole polybutycyanocrylate nanoparticles，ABZ-PBCA-NP）TDDS给药系统，并考察相关特性及组织分布靶向性。方法种子乳化聚合法制备阿苯达唑纳米粒；等温吸附法考察纳米粒载药特性；动态透析法研究4种制剂的体外释药动力学；同位素标记阿苯达唑纳米粒在小鼠脏器组织分布和生物利用度。结果ABZ-PBCA-NP体外释药遵循Higuchi方程，加入PVP制成的载药纳米粒符合双指数函数。纳米粒的载药方式遵循Langmuir吸附方程。小鼠ig ³H-ABZ-PBCA-NP后, 药物的肝、脾中的靶向指数分别为11.4和3.9，阿苯达唑纳米粒和混悬剂相对生物利用度分别为76.0%和36.9%。结论制备纳米粒加入PVP可使药物具吸附性和分散性，纳米粒载体可降低药物与血浆蛋白结合率，增强药物的肝、脾脏器靶向性和延缓释药。

Preparation of albendazole polybutycyanocrylate nanoparticles and study on its pharmaceutical properties and tissue distribution

Aim To prepare the targete drug delivery systems(TDDS), albendazole polybutycyanocrylate nanoparticles (ABZ-PBCA-NP), its pharmaceutical characters and tissue distributions were simultaneously investigated. Methods Albendazole nanoparticles were prepared with the emulsification-polymerization method and the drug-load mechanism of polybutycyanocrylate nanoparticles was studied with the equal-tempaerature adsorption principle. The dialyse dynamic of albendazole from ABZ-PBCA-NP was investigated in four formulations in vitro. The tissue distribution of albenda zole in different drug vehicles was studied with isotope labelling experiment. Results ABZ-PBCA-NP and ABZ-PVP-PBCA-NP fit to the Higuchi and bi-exponent function in vitro respectively. The drug loaded in nanoparticles was abide by the Langmuir adsorption equation. Targeting index of albendazole in liver and spleen in mice are 11 4 and 3 9 after ig 3H-ABZ-PBCA-NP. The bioavailability of albendazole nanoparticle and suspension are 76 0% and 36 9% respectively. Conclusion The absorptive capability of drug was enhance when 4% PVP was added into the nanoparticle, and its release time was lengthen. At the same time, the na noparticles vehicles increase the albendazole bioavailability.