Ursolic Acid Nanocrystals for Dissolution Rate and Bioavailability Enhancement: Influence of Different Particle Size

• DOI: 10.2174/1567201813666160307142757
• Publication Date: 2016-03-08T11:11:49Z
• Authors: Jiaxin Pi; Zhidong Liu; Hao Wang; Xing Gu; Shuya Wang; Bing Zhang; Hansen Luan; Zhuangzhi Zhu
• Keywords: 0303 health sciences; Calorimetry, Differential Scanning; Drug Compounding; Administration, Oral; Biological Availability; Triterpenes; Rats, Sprague-Dawley; 03 medical and health sciences; Drug Delivery Systems; Solubility; X-Ray Diffraction; Microscopy, Electron, Scanning; Pressure; Ursolic Acid; Animals; Nanoparticles; Particle Size; Powder Diffraction

Ursolic acid (UA), a natural pentacyclic triterpenoid, has been reported to possess variety of pharmacological activities, but the poor oral bioavailability UA owing aqueous solubility and membrane permeability limits further clinical application.The purpose present study was develop nanocrystals microcrystals employing high pressure homogenization (HPH) evaluate their effects on bioavailability.The crystalline morphology prepared by HPH observed scanning electron microscopy state characterized differential calorimetry (DSC) powder X-ray diffraction (PXRD). The dissolution rate in different pH conditions tested. Oral comparing with coarse suspension evaluated SD rats after 50 mg·kg-1 administration.UA microcrystals, size which ranged between 291.7 nm 1299.3 were obtained. results DSC PXRD revealed degree crystalline-amorphous transformation during preparation. A significant increase nanocrystals. relative exhibited 2.56 1.40-fold enhancement than that suspension, respectively, along an increased peak concentration prolonged retention.The nanosized crystal is viable efficient approach improve UA.