Zhang Xue-nong, Zhang Qiang, Wen Hao, Wang Guo-quan, Sun Dian-jia
Department of Pharmaceutics, School of Pharmaceutical Science, Peking University, Beijing 100083, China.
Yao Xue Xue Bao. 2003 Jun;38(6):462-6.
To prepare the target drug delivery systems(TDDS), albendazole polybutycyanocrylate nanoparticles (ABZ-PBCA-NP), its pharmaceutical characters and tissue distributions were simultaneously investigated.
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 albendazole in different drug vehicles was studied with isotope labelling experiment.
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.
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 nanoparticles vehicles increase the albendazole bioavailability.
制备阿苯达唑聚丁氰基丙烯酸酯纳米粒（ABZ-PBCA-NP）靶向给药系统，并对其药学性质及组织分布进行同步研究。
采用乳化聚合法制备阿苯达唑纳米粒，运用等温吸附原理研究聚丁氰基丙烯酸酯纳米粒的载药机制。体外考察了阿苯达唑在4种制剂中从ABZ-PBCA-NP的透析动力学。采用同位素标记实验研究了阿苯达唑在不同载药体系中的组织分布。
ABZ-PBCA-NP和ABZ-PVP-PBCA-NP在体外分别符合Higuchi方程和双指数函数。纳米粒中载药符合Langmuir吸附方程。小鼠灌胃3H-ABZ-PBCA-NP后，阿苯达唑在肝脏和脾脏中的靶向指数分别为11.4和3.9。阿苯达唑纳米粒和混悬液的生物利用度分别为76.0%和36.9%。
纳米粒中加入4%聚乙烯吡咯烷酮（PVP）可提高药物的吸附能力，延长其释放时间。同时，纳米粒载体提高了阿苯达唑的生物利用度。
