Zheng Yongli, Yang Wuli, Wang Changchun, Hu Jianhua, Fu Shoukuan, Dong Ling, Wu Lili, Shen Xizhong
Department of Macromolecular Science, Fudan University, and Zhongshan Hospital, Shanghai, China.
Eur J Pharm Biopharm. 2007 Nov;67(3):621-31. doi: 10.1016/j.ejpb.2007.04.007. Epub 2007 Apr 19.
New nonstoichiometric polyelectrolyte complex nanoparticles were prepared based on chitosan (CS) and polyaspartic acid sodium salt (PAsp). The physicochemical properties of the complexes were investigated by means of turbidity, dynamic light scattering, transmission electron microscopy and zeta potential. The results indicated that the slow dropwise addition of chitosan into PAsp allowed to elaborate either anionic or cationic particles in the size range of 85-300 nm with proper CS and PAsp unit molar ratios. Investigation of structural changes during the addition of CS revealed that the microstructure of the nanoparticles depended strongly on the unit molar ratio of CS to PAsp. Nanoparticles containing a hydrophilic drug, 5-fluorouracil (5FU), were prepared by mixing and absorption method. In vitro and in vivo experiment indicated that the drug-loaded CS-PAsp nanoparticles presented a sustained release of 5FU compared to the 5FU solution and the areas under curve (AUC) were increased by about four times.
基于壳聚糖（CS）和聚天冬氨酸钠盐（PAsp）制备了新型非化学计量聚电解质复合纳米粒子。通过浊度、动态光散射、透射电子显微镜和zeta电位对复合物的物理化学性质进行了研究。结果表明，将壳聚糖缓慢滴加到聚天冬氨酸中，可以制备出尺寸范围为85 - 300 nm的阴离子或阳离子颗粒，且壳聚糖和聚天冬氨酸单元摩尔比合适。对壳聚糖添加过程中结构变化的研究表明，纳米粒子的微观结构强烈依赖于壳聚糖与聚天冬氨酸的单元摩尔比。通过混合和吸附法制备了含有亲水性药物5-氟尿嘧啶（5FU）的纳米粒子。体外和体内实验表明，与5FU溶液相比，载药的CS-PAsp纳米粒子呈现出5FU的缓释特性，曲线下面积（AUC）增加了约四倍。
