Nitrendipine Nanocrystals: Its Preparation, Characterization, and In Vitro–In Vivo Evaluation

Abstract

The present investigation was undertaken with the objective of developing a solid formulation containing nitrendipine nanocrystals for oral delivery. Nitrendipine nanocrystals were prepared using a tandem precipitation–homogenization process. Then, spray drying, a cost-effective method very popular in industrial situations, was employed to convert the nanocrystals into a solid form. The parameters of the preparation process were investigated and optimized. The optimal process was as follows: firstly, nitrendipine/acetone solution (100 mg/ml) was added to a polyvinyl alcohol solution (1 mg/ml) at 10°C, then the pre-suspension was homogenized for 20 cycles at 1,000 bar. Both differential scanning calorimetry and X-ray diffraction analysis indicated that nitrendipine was present in crystalline form. The in vitro dissolution rate of the nanocrystals was significantly increased compared with the physical mixture and commercial tablet. The in vivo testing demonstrated that the C max of the nanocrystals was approximately 15-fold and 10-fold greater than that of physical mixture and commercial tablet, respectively. In addition, the AUC0→24 of the nanocrystals was approximately 41-fold and 10-fold greater than that of physical mixture and commercial tablet, respectively.

DOI: 10.1208/s12249-011-9682-2

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@article{Quan2011NitrendipineNI, title={Nitrendipine Nanocrystals: Its Preparation, Characterization, and In Vitro–In Vivo Evaluation}, author={Peng Quan and Dengning Xia and Hongze Piao and Hongyu Piao and Junying Shi and Yinnong Jia and Fude Cui}, journal={AAPS PharmSciTech}, year={2011}, volume={12}, pages={1136-1143} }