Preparation and pharmaceutical characteristics of naringenin nanocrystals / 中草药

ABSTRACT

Objective: To prepare and investigate the pharmaceutical characteristics of naringenin (NAR) nanocrystals. Methods: NAR nanocrystals were prepared by media milling combined with spray drying method. The mean particle size and polydispersity index (PDI) of NAR nanocrystals were analyzed by Malvern Zetasizer. The morphology of the nanoparticles was observed by scanning electron microscope (SEM). The crystalline state and the chemical structure of NAR before and after nanonization were characterized using X-ray powder diffraction (XRPD), differential scanning calorimetry (DSC), and fourier transform infrared spectrometry (FT-IR). Dissolution rate of NAR before and after nanonization were studied using rotary basket method. Results: The mean particle size of NAR nanocrystals was (400.7 ± 6.9) nm, and PDI value was 0.23. After nanonization, the crystalline state and chemical structure of NAR were not obviously altered, and the solubility was significantly increased (in pH 1.2 hydrochloric acid solution and pH 4.5 phosphate solution, P < 0.05; in pH 6.8 phosphate solution and water, P < 0.01). The dissolution was obviously improved, T50 and Td were visibly decreased (P < 0.01). Conclusion: The optimized process is stable and feasible for the preparation of NAR nanocrystals. NAR nanocrystals have a tiny and uniform particle size. After nanonization, NAR was still crystalline, the solubility and the dissolution were significantly increased, which can provide the basis for the further development of NAR.