米托蒽醌聚氰基丙烯酸正丁酯毫微粒的研究

STUDY ON MITOXANTRONE POLYCYANOACRYLATE NANOSPHERES

用乳化聚合法制备了米托蒽醌聚氰基丙烯酸正丁酯毫微粒，并对其表面荷电特性、形态、大小及其分布、体外释药性质、载药量、初步稳定性和在动物体内的分布进行了研究。结果表明，粒径ｄａｖ＝５５．２３ｎｍ，载药量为４６．７７％，包封率为８４．８９％，表面带负电荷。体外释药符合双相动力学规律。其胶体溶液能经受煮沸３０ｍｉｎ灭菌。经氚标记液闪计数技术测定证实其ｉｖ后主要集中于肝脏，并有一定的肝肿瘤和肝细胞的靶向性。提示其对于提高米托蒽醌抗肝癌的效果和降低其全身毒副作用有重要意义。

The mitoxantrone polybutylcyanoacrylate nanosparticles( DHAQ-PBCA-NP )wereprepared by emulsion polymerization method. The surface charge,drug lodaing,morphology, sizeand size distribution, release characteristics in vitro,stablity and distribution in animals of DHAQ-PR-CA-NP were studied. The results showed that the mean size wasdav=55.23 nm,drug loading was46.77%,embedding ratio was 84.89%. The surface carried negative charge and the release charac-teristics in vitro was in accord with two phases kinetics law. The colloidal solution Of DHAQ-PECA-NPcan undergo boilling for 30 min sterilization. The radiOactivity concentrated mainlv in liver after iv3H-DHAQ-PBCA-NP. The radioactivity in liver tumor was higher than that in the liver tissue.DHAQ-PBCA-NP was observed in parenchymal cell 15 min after iv DHAQ-PBCA-NS.This prepara-tion seems to have important value for increasing the anti-liver tumor effect and decreasing the toxicityof DHAQ.