乳酸-羟基乙酸共聚物载药纳米粒的制备及体外释药性

摘要 背景：医用纳米粒作为药物传递的新型载体，目前已经成为医药领域研究的重点。 目的：构建以生物可降解材料乳酸-羟基乙酸共聚物为载体，负载抗肿瘤药物5-氟尿嘧啶的载药纳米粒。 方法：利用复乳-溶剂挥发法制备乳酸-羟基乙酸共聚物载药纳米粒。场发射扫描电子显微镜观察纳米粒表面形态；激光粒度分析仪测定粒径分布并计算成球率；紫外分光光度计测定5-氟尿嘧啶载药量、包封率，并对体外释药进行评估。 结果与结论：纳米粒呈球性，平均粒径为(186±14) nm，成球率、载药量和包封率分别为70.8%、6.6%、28.1%，体外释药有突释现象，24 h内5-氟尿嘧啶累积释药量达36.2%，10 d达83.6%。提示成功制备乳酸-羟基乙酸共聚物载药纳米粒，其具有缓释效应。 关键词：乳酸-羟基乙酸共聚物；5-氟尿嘧啶；纳米粒；体外释药；缓释 doi:10.3969/j.issn.1673-8225.2011.16.017

Preparation of drug-loaded poly (D, L-lactide-co-glycolide) nanoparticles and characterization of release behavior in vitro

Abstract BACKGROUND: As a new drug delivery carrier, medical nanoparticle has currently become the focus of research in the field of medicine. OBJECTIVE: To construct antitumor drug 5-fluorouracil (5-FU) loaded nanoparticles using the biodegradable material poly (D, L-lactide-co-glycolide) (PLGA). METHODS: The PLGA nanoparticles were prepared by double emulsification solvent evaporation technique. The morphology and particle size distribution of nanoparticles were determined by field emission scanning electron microscope and laser particle size analyzer, respectively, and the granulation rate of nanoparticles was calculated. The drug loading, encapsulation efficiency of 5-FU and release in vitro were detected by ultraviolet spectrophotometer. RESULTS AND CONCLUSION: The nanoparticles were spherical in shape with average diameter (186±14) nm. The granulation rate, drug loading and encapsulation efficiency was 70.8%, 6.6%, 28.1%, respectively. The nanoparticles exhibited initial burst release in vitro, releasing a cumulative 36.2% of 5-FU in 24 hours. The cumulative release reached 83.6% at the 10th day. The results suggested that the 5-FU-loaded PLGA nanoparticles were prepared successfully and have slow release function in vitro.