半乳糖化阿霉素白蛋白纳米粒的制备及其质量评价  

Preparation and evaluation of galactosyl adriamycin BSA nanoparticles

作　　者：王旭波[1] 徐希明[2] 葛亮[1] 丁妍[2] 张钧寿[1] 

机构地区：[1]中国药科大学药剂系,南京210009 [2]江苏大学药学院,镇江212001

出　　处：《中国新药杂志》2005年第7期870-872,共3页Chinese Journal of New Drugs

基　　金：江苏省自然科学基金资助项目(BK99193);江苏省青年科技基金资助项目(BQ2000012)

摘　　要：目的:制备半乳糖化阿霉素白蛋白纳米粒,并考察了其形态、粒径、载药量、包封率和体外释药特性。方法:采用相分离法制备阿霉素白蛋白纳米粒,并在其表面偶联半乳糖苷,使之成为半乳糖化白蛋白纳米粒。激光扫描电子显微镜观察纳米粒的形态,马尔文激光粒度仪测定其粒径分布。采用紫外分光光度法测定纳米粒的载药量和包封率,并初步研究其体外释药特性。结果:电镜结果显示阿霉素纳米粒呈类球型,平均粒径为316·3nm,纳米粒载药量为3·12%,包封率达91·82%,48h体外累积释药率为55·71%。结论:本方法制备阿霉素纳米粒工艺简单且包封率较高。体外释药结果显示半乳糖化阿霉素白蛋白纳米粒具有明显的缓释作用。Objective：To prepare and characterize the adriamycin nanoparticles coupling with a carrier material bovine serum albumin （BSA） as well as galactose. Methods：Adriamycin nanoparticles （ABN） were prepared by phase separation technique using BSA as carrier materials, and galactosyl BSA nanoparticles （GBN） were then formulated by complexing galactose onto the surface of the BSA nanoparticles. Scanning electron microscopy was used to assess the shape of the nanoparticles. Malveru Zeta Nano-ZS was performed to measure the particle size distribution.The drug loading （DL） and trapping efficiency （DTE）, as well as the drug release characteristic in vitro were investigated with UV spectrophotometry. Results： The study results showed that the GBN were spherical with an average diameter of 316.3 nm. The DL and DTE was 3.12% and 91.82 %, respectively.55.71% of adriamycin could be released from GBN over a period of 48 h. Conclusion： The formulation method presented here was simple with a high DTE, and made the GBN provide a sustained release of adriamycin in vitro.

关 键 词：半乳糖化 阿霉素 纳米粒 质量评价 

分 类 号：R944.9[医药卫生—药剂学] R979.14[医药卫生—药学]