Preparation and In Vitro Drug-Release Behavior of 5-Fluorouracil-Loaded Poly(hydroxybutyrate-co-hydroxyhexanoate) Nanoparticles and Microparticles
Preparation and In Vitro Drug-Release Behavior of 5-Fluorouracil-Loaded Poly(hydroxybutyrate-co-hydroxyhexanoate) Nanoparticles and Microparticles
复制标题
5-氟尿嘧啶聚羟基丁酸酯-羟基己酸酯纳米粒和微粒的制备及其体外释药行为
DOI：
10.1002/app.31806
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发表时间：
2010-06-05
影响因子：
3
通讯作者：
Wang, Liang
中科院分区：
文献类型：
--
作者：
Lu, Xiao-Yun;Zhang, Yali;Wang, Liang
采用双乳液溶剂蒸发技术制备了聚（3-羟基丁酸酯-co-3-羟基己酸酯）（PHBHHx）共聚微粒子（MPs）和纳米粒子（NPs）。5-氟尿嘧啶（5-Fu）是一种抗癌药物，被包裹在PHBHHx NPs和MPs中。研究了不同表面活性剂的种类和浓度、超声波对颗粒分散的功率和时间、有机/水溶液比等参数对负载5-Fu的PHBHHx NP和MP颗粒的生成及5-Fu的释放的影响。结果表明，以十六烷基三甲基溴化铵为乳化剂时，制备的NPs和MPs为球形，尺寸分别约为160 nm和3 μ m。5-Fu对NPs和MPs的载药量影响较大，分别为3.53 ~ 8.03%和4.83 ~ 18.87%。随着DLC的增加，封装效率降低。体外释药特征表现为两个阶段，最初的爆发效应发生在前8 h；这在dlc较低的粒子中更为明显。DLC高的NPs（8.03%）在24 h内释放5-Fu的速度最慢，为49.6%。因此，PHBHHx共聚NPs和MPs有可能在未来作为给药载体材料。(C) 2010 Wiley期刊公司高分子学报（英文版），2010
Poly(3-hydroxybutyrate-co-3-hydroxyhexanoate) (PHBHHx) copolymeric microparticles (MPs) and nanoparticles (NPs) were prepared by the double-emulsion solvent-evaporation technique. 5-Fluorouracil (5-Fu), an anticancer drug, was entrapped in PHBHHx NPs and MPs. A variety of parameters, including the species and concentration of different surfactants, power and time of ultrasonication for particle dispersion, and organic/aqueous solution ratio, that affected the production of the 5-Fu-loaded PHBHHx NP and MP particles and the release of 5-Fu were studied. The results show that the prepared NPs and MPs were spherical in shape and about 160 nm and 3 mu m in size, respectively, when cetyltrimethyl ammonium bromide was used as the emulsifier. The drug-loading content (DLC) varied from 3.53 to 8.03% for 5-Fu-loaded NPs and from 4.83 to 18.87% for 5-Fu-loaded MPs and depended on the different initial feeding amounts of 5-Fu. The encapsulation efficiency decreased with increasing DLC. The in vitro drug-release characteristics appeared to have two phases with an initial burst effect occurring within the first 8 h; this was more obvious for the particles with low DLCs. The NPs with high DLC (8.03%) had the slowest release rate, 49.6% of 5-Fu within 24 h. Therefore, PHBHHx copolymeric NPs and MPs can possibly be applied as drug-delivery carrier materials in the future. (C) 2010 Wiley Periodicals, Inc. J Appl Polym Sci 116: 2944-2950, 2010