A novel surface modified nitrendipine nanocrystals with enhancement of bioavailability and stability

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• 作者：Peng Quan ; Kai Shi ; Hongze Piao ; Hongyu Piao ; Na Liang ; Dengning Xia ; Fude Cui ; ^{cuifude@163.com}
• 关键词：Chitosan ; Nitrendipine ; Nanocrystal ; Dissolution ; Bioavailability
• 刊名：International Journal of Pharmaceutics
• 出版年：2012
• 期刊代码：24_03785173
• 类别：pha
• 出版时间：1 July, 2012
• 卷：430
• 期：1-2
• 页码：366-371
• 文件大小：823 K

摘要

In this study, chitosan, a cationic polymer with positive charge, was introduced to modify the nanocrystals of nitrendipine with negative charge. The nanocrystals were prepared via precipitation-high pressure homogenization method. Then the nanocrystals were dispersed into chitosan solution, and the free chitosan was removed by centrifugation to obtain the chitosan modified nanocrystals, which remained the same particle size. However, the zeta-potential changed to positive after modification.

The physical stability of the chitosan modified nanocrystals was remarkably improved under ambient conditions. During the in vitro dissolution test, the modified nanocrystals showed a certain degree of slow-release property. In the in vivo study, the C_max of nitrendipine remained the same, however, the T_max delayed from 0.75 h to 1.5 h with the chitosan modified nanocrystals. The surface modification by chitosan improved the bioavailability compared with the initial nanocrystals, which had demonstrated significant improvement of bioavailability compared to the traditional coarse powder form. Based on the experimental results, modification of the nanocrystals with certain polymer was supposed to be a good method to control the in vitro and in vivo behaviors of the nanocrystals, which could further increase the bioavailability of the water insoluble drug.