摘要
目的制备具有酸敏特性的聚(甲基丙烯酸缩水甘油酯修饰葡聚糖,dex-GMA)/(丙烯酸,AAc)纳米凝胶,研究其降解和释药性质。方法乳液聚合法制备poly(dex-GMA/AAc)纳米凝胶,测定不同pH值下的粒度分布,以红霉素(EM)为药物模型,动态透析法测定纳米凝胶在不同pH值下的释药性质。结果poly(dex-GMA/AAc)纳米凝胶的平均粒径约为100 nm,包裹率、载药率分别为90.7%和1.06%。在无酶人工胃液(SGF)2 h纳米凝胶的药物累积释放率分别为7.0%,之后在无酶人工肠液(SIF)里4 h内增加到37.0%。结论poly(dex-GMA/AAc)纳米凝胶具有酸敏特性,在SGF里释放少量药物,在SIF里凝胶溶胀、降解,药物释放量明显增大。poly(dex-GMA/AAc)纳米凝胶是潜在的结肠靶向载体。
Objective To prepare the pH -sensitive glycidyl methacrylate derivatized dextran (dex-GMA)/acrylic acid (AAc) poly(dex-GMA/AAc) nanoparticles, and study their properties such as drug release and degradation. Methods The poly (dex-GMA/AAc) nanoparticles were prepared by emulsion polymerization. Under different pH, the particle size distribution and drug release of poly (dex-GMA/AAc) nanoparticles were determined by dynamic dialysis methods with erythromycin as a drug model. Results The mean diameter of poly(dex-GMA/AAc) nanoparticles was about 100 nm, the drug loading rate and encapsulation efficiency were 90.7%, and 1.06%, respectively. In the artificial gastric fluid without enzymes(SGF) , the cumulative drug release ratio was 7.0% within 2 h, afterwards reached to 37.0% within 4 h in the artificial intestinal fluid (SIF) without enzymes. Conclusion The poly (dex-GMA/AAc) nanoparticles were pH-sensitive, which released EM slightly in SGF, whereas released considerably more in SIF by swelling and degradating. It is suggested that the poly (dex-GMA/AAc) nanoparticle would be a potential colon-target carrier.
出处
《医药导报》
CAS
2008年第8期967-970,共4页
Herald of Medicine
基金
国家自然科学基金资助项目(基金编号:30770573)
全军医药卫生科研基金资助项目(基金编号:06Q064)
关键词
葡聚糖
纳米凝胶
乳液聚合
酸敏
Dextran
Nanoparticles
Emulsion polymerization
PH-sensitive
作者简介
张慧(1981-),女,山东泰安人,在读硕士,研究方向:智能纳米药物载体。电话:029—82502058,E—mail:zhhui58@hotmail.com。
[通讯作者]吴红(1971-),女,陕西西安人,硕士生导师,副教授,主要从事智能纳米药物载体研究。电话:029—84774473—800,E—mail:renlei@fmmu.edu.cn。