中国组织工程研究2012，Vol.16Issue(29)：5331-5335,5.DOI:10.3969/j.issn.2095-4344.2012.29.003
马钱子碱免疫纳米微粒的研制及药代动力学特点
Preparation and pharmacokinetics of brucine immuno-nanoparticles
摘要
Abstract
BACKGROUND: Brucine is highly toxic and insoluble in water, as well as has narrow intravenous therapeutic window. The amount of poisoning and treatment is close. Therefore, brucine is limited in clinical treatment of liver cancer and other malignant tumors. OBJECTIVE: To prepare the brucine immuno-nanoparticles and to observe the characteristics of the drug metabolism in vivo. METHODS: Anionic polymerization and chemical modification technology were used to prepare carboxylated polyethylene glycol-poly lactic acid copolymer. Phacoemulsification technology was employed to prepare carboxylated polyethylene glycol-polylactic acid copolymer brucine nanoparticles. Then, chemical coupling technology was utilized to combine the anti-human alpha-fetoprotein monoclonal antibody with the polyethylene glycol-poly lactic acid copolymer brucine nanoparticles to prepare the brucine immuno-nanoparticles with immune targeting. RESULTS AND CONCLUSION: Brucine immuno-nanoparticles showed uniform size with an average particle size of (249?7) nm and Zeta potential of (-18.7?.19) mV. The encapsulation efficiency was (76.0?.3)% and the drug load was (5.6?.2)%. Brucine immuno-nanoparticles were very stable in the medium with an accumulative release rate of over 80% in 24 hours and 100% in 48 hours. Brucine immuno-nanoparticles belonged to non-compartment model during in vivo metabolic process. The half life period of brucine immuno-nanoparticles was (15.69?.77) hours, which was longer than that of the brucine (P < 0.01). The brucine immuno-nanoparticles with immune targeting are successfully prepared that belong to non-compartment model during in vivo metabolic process, and show sustained-release properties.关键词
马钱子碱/免疫纳米微粒/制备/药代动力学/生物材料分类
医药卫生引用本文复制引用
秦建民,陈庆华,马经纬,沈鹤柏,杨林,撒忠秋,黄涛,盛霞,李琦,殷佩浩,张敏,高科攀..马钱子碱免疫纳米微粒的研制及药代动力学特点[J].中国组织工程研究,2012,16(29):5331-5335,5.基金项目
上海市教委项目(07CZ017) （07CZ017）
上海市科委项目(1052nm06000) （1052nm06000）
国家自然科学基金资助项目(30873341). （30873341）
