Membrane-encased polymer millirods for sustained release of 5-fluorouracil
Membrane-encased polymer millirods for sustained release of 5-fluorouracil
复制标题
DOI：
10.1002/jbm.10156
复制
发表时间：
2002-08-01
期刊：
影响因子：
--
通讯作者：
Gao, JM
中科院分区：
文献类型：
--
作者：
Qian, F;Nasongkla, N;Gao, JM
本文介绍了一种新型的膜包裹的聚合物毫米棒的抗癌药物，5-氟尿嘧啶（5-FU）的持续释放的设计和开发。毫米棒由两个功能隔室组成：（1）内部5-FU装载的单片毫米棒作为药物贮库，以及（2）外部NaCl浸渍的聚合物膜以控制5-FU的释放速率。通过压缩-加热成型程序制造内部毫米棒，以允许将5-FU颗粒截留在聚（D，L-丙交酯-共-乙交酯）（PLGA）基质中。将载药密度控制在30 w/w%，以实现5-FU从单片毫杆的突释（>90%的药物在48小时内释放）。NaCl浸渍的PLGA膜通过溶剂浇铸产生，然后包裹在单片毫杆上以产生膜包裹的毫杆。扫描电子显微镜显示，NaCl颗粒的溶解产生半渗透性聚合物膜，以提供5-FU的持续释放。膜厚度和膜内NaCl颗粒的密度是控制5-FU释放动力学的有用参数。在本研究的实验条件下，5-FU的缓释[速率在0.1和0.4 mg/（天）之间。cm毫罗德）]在磷酸盐缓冲盐水（pH7.4）中于37 ℃下进行2至5周。本研究的结果表明，膜包裹的聚合物毫杆提供可控的持续释放动力学的肿瘤内药物输送的应用。(C)2002 Wiley Periodicals，Inc.
This article describes the design and development of a novel membrane-encased polymer millirod for the sustained release of an anticancer drug, 5-fluorouracil (5-FU). The millirod consists of two functional compartments: (1) an inner 5-FU-Ioaded monolithic millirod as the drug depot, and (2) an outer NaCl-impregnated polymer membrane to control the release rate of 5-FU. The inner millirod is fabricated by a compression-heat molding procedure to permit the entrapment of 5-FU particles in the poly(D,L-lactide-co-glycolide) (PLGA) matrix. The drug loading density is controlled at 30 w/w% to achieve a burst release of 5-FU (>90% of the drug are released within 48 h) from the monolithic millirod. The NaCl-impregnated PLGA membrane is generated by solvent casting and is then wrapped over the monolithic millirod to produce the membrane-encased millirod. Scanning electron microscopy shows that dissolution of NaCl particles produces a semipermeable polymer membrane to provide a sustained release of 5-FU. The membrane thickness and the density of NaCl particles inside the membrane are useful parameters to control the release kinetics of 5-FU. Under the experimental conditions in this study, sustained release of 5-FU [rates between 0.1 and 0.4 mg/(day . cm of millirod)] is achieved for 2 to 5 weeks in phosphate-buffered saline (pH 7.4) at 37degreesC. Results from this study demonstrate that membrane-encased polymer millirods provide controllable sustained release kinetics for applications in intratumoral drug delivery. (C) 2002 Wiley Periodicals, Inc.