Hot melt extrusion aided amorphous solid dispersions of quercetin and resveratrol for solubility enhancement

Lakshmi Swapna Sai; Fatima S  Dasankoppa; Srinivas Mutalik; Muralidhar Pisay

doi:10.69857/joapr.v13i1.734

Authors

Lakshmi Swapna Sai Department of Pharmaceutics, KLE College of Pharmacy, Vidyanagar, Hubballi (A constituent unit of KLE Academy of Higher Education and Research, Belagavi), Karnataka, India - 580031 https://orcid.org/0000-0001-6439-2048
Fatima S Dasankoppa Department of Pharmaceutics, KLE College of Pharmacy, Vidyanagar, Hubballi (A constituent unit of KLE Academy of Higher Education and Research, Belagavi), Karnataka, India - 580031
Srinivas Mutalik Department of Pharmaceutics, Manipal College of Pharmaceutical Sciences, Manipal Academy of Higher Education, Manipal, Karnataka, India 576104
Muralidhar Pisay Department of Pharmaceutics, Manipal College of Pharmaceutical Sciences, Manipal Academy of Higher Education, Manipal, Karnataka, India 576104

DOI:

https://doi.org/10.69857/joapr.v13i1.734

Keywords:

Hot melt extrusion, Amorphous solid dispersion, Soluplus, Quercetin, Resveratrol, Kolliphor, Polyvinylpyrrolidone

Abstract

Background: Conversion of poorly soluble drugs into amorphous solid dispersions using different carriers is a formulation approach to improve solubility. Objective: The study investigates hot melt extrusion as an approach for producing amorphous solid dispersions that contribute to solubility enhancement. Methodology: Solid dispersions were hot melt extruded using two model compounds – quercetin and resveratrol with different carriers. The resulting solid dispersions were analyzed for solubility enhancement and characterized by various techniques. Results and Discussion: The solubility of solid dispersions was evaluated, revealing a 36-fold increase in the solubility of quercetin from 0.023 mg/ml to 0.823 mg/ml and a 97-fold increase in the solubility of resveratrol from 0.053 mg/ml to 5.125 mg/ml with soluplus as a carrier. Various characterization studies indicated the conversion of crystalline forms of quercetin and resveratrol into their amorphous forms, which was confirmed by powder x-ray crystallographic and scanning electron microscopic studies. In addition, the particle size reduction of quercetin reduced from 1.53 μm to 0.48 μm and resveratrol of 10.26 μm particle size was reduced to 0.22 μm in solid dispersions with soluplus as the carrier with decreased polydispersity index. Conclusion: This research demonstrates hot melt extrusion as a practical approach for fabricating amorphous solid dispersions.

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