Soluplus-Mediated Diosgenin Amorphous Solid Dispersion with High Solubility and High Stability: Development, Characterization and Oral Bioavailability

Liu P, Zhou J, Chang J, Liu X, Xue H, Wang R, Li Z, Li C, Wang J, Liu C
2020 Drug Design, Development and Therapy  
Pei Liu,1,2 Jian-yu Zhou,2 Jin-hua Chang,2 Xi-gang Liu,2 He-fei Xue,2 Ru-xing Wang,2 Zhong-si Li,2 Chun-shi Li,3 Jian Wang,3 Cui-zhe Liu1,2 1Department of Pharmaceutics, School of Pharmacy, Shenyang Pharmaceutical University, Shenyang 110016, People's Republic of China; 2Hebei Province Key Laboratory of Research and Development for Chinese Medicine, Chengde Medical University, Chengde, Hebei 067000, People's Republic of China; 3Key Laboratory of Structure-Based Drug Design & Discovery of
more » ... y of Education, Shenyang Pharmaceutical University, Shenyang 110016, People's Republic of ChinaCorrespondence: Cui-zhe Liu 103 Wenhua Road, Shenyang 110016, People's Republic of ChinaTel +86-0314-2291142Email liucuizhexy@163.comJian WangHebei Province Key Laboratory of Research and Development for Chinese Medicine, Chengde Medical University, Chengde, Hebei 067000, People's Republic of ChinaTel +86-13604051904Email jianwang@email.comBackground and Purpose: The traditional Chinese medicine, diosgenin (Dio), has attracted increasing attention because it possesses various therapeutic effects, including anti-tumor, anti-infective and anti-allergic properties. However, the commercial application of Dio is limited by its extremely low aqueous solubility and inferior bioavailability in vivo. Soluplus, a novel excipient, has great solubilization and capacity of crystallization inhibition. The purpose of this study was to prepare Soluplus-mediated Dio amorphous solid dispersions (ASDs) to improve its solubility, bioavailability and stability.Methods: The crystallization inhibition studies were firstly carried out to select excipients using a solvent shift method. According to solubility and dissolution results, the preparation methods and the ratios of drug to excipient were further optimized. The interaction between Dio and Soluplus was characterized by differential scanning calorimetry (DSC), fourier transform infrared (FT-IR) spectroscopy, scanning electron microscopy (SEM), powder X-ray diffraction (PXRD) and molecular docking. [...]
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