Optimization and evaluation of resveratrol amorphous solid dispersions with a novel polymeric system

Author:

Han Gangqi123,Wang Bing34,Jia Mengli3,Ding Shuxin3,Qiu Wenxuan3,Mi Yuxuan3,Mi Zhimei3,Qin Yuhao3,Zhu Wenxing12,Liu Xinli12,Li Wei5

Affiliation:

1. State Key Laboratory of Bio-based Material and Green Papermaking (LBMP), Qilu University of Technology (Shandong Academy of Sciences), Jinan, Shandong, China

2. Key Laboratory of Shandong Microbial Engineering, School of Bioengineering, Qilu University of Technology (Shandong Academy of Sciences), Jinan, Shandong, China

3. College of Pharmacy, Heze University, Heze, Shandong, China

4. Shandong Dashu Dafute Food Co., Ltd, Heze, Shandong, China

5. Shandong Medical College, Jinan, Shandong, China

Abstract

<abstract> <p>The preparation of amorphous solid dispersions using polymers is a commonly used formulation strategy for enhancing the solubility of poorly water-soluble drugs. However, a single polymer often does not bring significantly enhance the solubility or amorphous stability of a poorly water-soluble drug. We found an application of a unique and novel binary polymeric blend in the preparation of solid dispersions. The main purpose of this study is to optimize and evaluate resveratrol (Res) amorphous solid dispersions with a novel polymeric system of poly (vinyl pyrrolidone) (PVP) and carboxymethyl chitosan (CMCS). The influence of three different release factors, the ratio of CMCS to the polymer mixture (CMCS% = X<sub>1</sub>), the ratio of Res to the polymer mixture (Res% = X<sub>2</sub>) and the surfactant (Tween 80 = X<sub>3</sub>), on the characteristics of released Res at various times (Q<sub>5</sub> and Q<sub>30</sub>) was investigated. The computer optimization and contour plots were used to predict the levels of the independent variables as X<sub>1</sub> = 0.17, X<sub>2</sub> = 0.10 and X<sub>3</sub> = 2.94 for maximized responses of Q<sub>5</sub> and Q<sub>30</sub>. Fourier transform infrared spectroscopy (FTIR) results revealed that each polymer formed hydrogen bonds with Res. The solid performance and physical stability of the optimized ternary dispersions were studied with scanning electron microscopy (SEM), powder X-ray diffraction (XRD), modulated differential scanning calorimetry (MDSC) and dissolution testing. SEM, XRD and MDSC analysis demonstrated that the Res was amorphous, and MDSC showed no evidence of phase separation during storage. Dissolution testing indicated a more than fourfold increase in the apparent solubility of the optimized ternary dispersions, which maintained high solubility after 90 days. In our research, we used CMCS as a new carrier in combination with PVP, which not only improved the <italic>in vitro</italic> dissolution of Res but also had better stability.</p> </abstract>

Publisher

American Institute of Mathematical Sciences (AIMS)

Subject

Applied Mathematics,Computational Mathematics,General Agricultural and Biological Sciences,Modeling and Simulation,General Medicine

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