羟基喜树碱叶酸-壳聚糖纳米粒的制备及其性能研究  

Preparation and characterization of hydroxycamptothecin loated folate-chitosan nanoparticles as a sustained-release drugs carrier

作　　者：邢志华[1,2] 方桂珍[1] 苏玲[1] 李津明[2] 

机构地区：[1]东北林业大学材料科学与工程学院,黑龙江哈尔滨150040 [2]哈尔滨商业大学药学院,黑龙江哈尔滨150076

出　　处：《功能材料》2012年第B11期322-325,共4页Journal of Functional Materials

基　　金：教育部博士学科点基金资助项目(20060225008)

摘　　要：为了提高羟基喜树碱对肿瘤组织的靶向性,增强其抗肿瘤活性,延长其在体内的作用时间,以壳聚糖为药物载体,叶酸为肿瘤靶向配体,三聚磷酸钠为聚阴离子,利用静电相互作用的原理,通过离子交联法合成载羟基喜树碱的叶酸-壳聚糖(FA-CTS/HCPT)纳米粒。利用动态光散射、透射电镜以及红外等技术对纳米粒的结构、平均粒径及粒径分布、形态特征、表面电位、稳定性、对药物的包封率及载药量、体外释放等特点进行了初步研究。结果表明,所制得的纳米粒平均粒径为150nm;粒子形态圆整,大小均匀;表面电位+50.1mV;放置数十天纳米粒粒径几乎无变化,纳米粒具有很好的粒度稳定性;对羟基喜树碱包封率最高为89.9%,载药量最高为19.8%;在人工体液pH值为7.4条件下具有很好的缓释作用,用Higuchi方程拟合其体外释放曲线,得Higuchi方程:Q=14.529t1/2+8.3589(R2=0.9247),说明HCPT在人工体液的释放量与时间的平方根成直线关系,符合水不溶性骨架的释药性能。In order to enhance the tumor-targeting and anticancer activity of hydroxycamptothecin （HCPT）, and extend the in vivo effect of time, hydroxycamptothecin-loaded nanoparticles made from folate （FA）-decorated chitosan （CTS） were prepared and their release characteristics in vitro was evaluated. FA-CTS/HCPT nanoparticles were prepared by the ionic crosslinking method through the electrostatic interaction between the protonated amino of chitosan in acidic conditions and the deprotonation of carboxyl of folic acid in alkaline conditions as well as trimeric sodium phosphate （TPP）. The morphological characteristics of nanoparticles were examined using a transmitting electron microscope （TEM）. The average diameter of nanoparticles and size distribution were determined by dynamic light scattering. The drug encapsulation efficiency （EE）,loading capacity （LC）, and in vitro release characteristics were determined using ultraviolet spectrophotometer. The results indicated that the nanoparticles are uniform spherical and regular, with a size of 150nm, q-50. lmV surface potential and good size stability. Its encapsulation efficiency and loading capacity were up to 89.9% and 19.8 % respectively. The Higuchi equation Q= 14. 529t1/a -t-8. 3589 （R^2 = 0. 9247）can well describe release curve of the FA-CTS/ HCPT nanoparticles in vitro（PBS Buffer solution of pH=7.4）.

关 键 词：壳聚糖 纳米粒 羟基喜树碱 离子交联 肿瘤靶向 

分 类 号：R944.9[医药卫生—药剂学] O175.14[医药卫生—药学]