β-雌二醇纳米粒的制备及其肝脏靶向性的动物实验  

Study on liver targeting of estradiol polybutylcyanoacrylate nanoparticles

作　　者：全俊[1] 周建亮[1] 谢建萍[1] 肖平[2] 潘一峰[2] 

机构地区：[1]中南大学湘雅医院感染病科,长沙410008 [2]卫生部纳米生物技术重点实验室

出　　处：《中华传染病杂志》2008年第2期78-80,共3页Chinese Journal of Infectious Diseases

基　　金：湖南省自然科学基金资助项目（03JJY3060）

摘　　要：目的制备β-雌二醇聚氰基丙烯酸正丁酯纳米粒（E2纳米粒），观察E2纳米粒在正常小鼠肝脏中的靶向性。方法以聚氰基丙烯酸正丁酯（PBCA）为载体，优化制备条件，采用界面聚合法制备E2纳米粒，采用放射示踪技术，用地125^I标记雌二醇后，制备125^I-E2纳米粒，分别经腹腔及静脉给药，于不同时间点处死120只小鼠，取其血、肺、肝、脾、肾和子宫，测其放射性，并与普通雌二醇（E2）比较E2纳米粒在不同组织的分布情况。数据行单因素方差分析。结果制备E2纳米粒的最佳条件为800r／min，E25mg，PBCA0．6mL，丙酮45mL，Pluronic F-680．75％。以此条件制备纳米粒主要分布在50～180nm，平均粒径为115nm，包封率为90．3％。125^I-E2纳米粒和125^I-E2的肝摄取在注射后15min达高峰，与125^I-E2比较，125^I-E2纳米粒提高了肝脏、脾脏的放射性强度，其靶向指数分别为4.40±4．06和1．20±0．49，子宫及卵巢的放射性强度低。结论E2以PBCA作为载体，制成纳米药物后具有明显的肝靶向性。Objective To prepare beta-estradiol polybutylcyanoacrylate nanoparticles（E2 nanoparticles）, and observe its hepatic targeting. Methods E2 nanoparticles were prepared by interracial polymerization with the butylcyanoacrylate as its carrier. Using radioactive tracer technique, estradiol （E2） was labelled with 125^I, 125^I-E2 nanopartieles was also prepared by interracial polymerization and was injected into mouse by intraperitoneal injection and intravenous injection. The mice were sacrificed at different time points after injection. The radioactivity of blood, lung, liver, spleen, kidney, and uterus was analyzed by γ counts. Results The optimized conditions for preparing E2 nanoparticles were 800 r/min, E2 5 mg, polybutylcyanoacrylate 0. 6 mL, acetone 45 mL and Pluronic F-68 0.75%. The distribution of 125^I-E2 nanoparticles was between 50- 180 nm, and the ratio of enveloping was 90.3%. The concentrations of 125^I-E2 nanoparticles and 125^I-E2 reached the peak in liver at 15 min after administration of drugs. The radioactivity of 125^I-E2 nanoparticles in liver and spleen increased as compared with 125^I-E2, with drug targeting index reaching 4.40 ± 4.06 and 1.20 ± 0.49 respectively. Meanwhile, the radioactivity in ovary and uterus decreased. Conclusion E2 nanoparticles show remarkable hepatic targeting in rat model.

关 键 词：雌二醇 纳米技术 肝靶向性 

分 类 号：R943[医药卫生—药剂学]