Solubility Enhancement of BCS Classified II/IV Drug – Solid Dispersion of Apixaban by Solvent Evaporation

Abstract

Background: Solubility is an important physico-chemical factor affecting absorption of drug and its therapeutic effectiveness. One of the major problems responsible for the low turnout in the development of new molecular entities as drug formulations is poor solubility and poor permeability of the lead compounds. Objectives: The present research work was aimed to enhance the solubility of Apixaban drug by using Solid Dispersion Technique. Methods: The solid dispersion is the technique for the formulation of water insoluble drugs to enhance their aqueous solubility, absorption as well as dissolution rate, which leading to enhancement of bioavailability of drugs as compared to conventional directly compressed tablets. In this study, Apixaban was opted for formulating Solid dispersion with Hydrophilic polymers like HPMC E50 LV, HPMC E5, PEG 6000 and PVP K-30 by Spray drying method using a structured I optimal screening DOE. To screen out the ratio of polymer and suitable polymer type for solid dispersion resulted into highest solubility as a response. Results: The Solid dispersion of Apixaban showed improvement in the solubility in water by multiple folds when Apixaban used in combination with Hydrophilic polymers. The Apixaban solid dispersion with polymer HPMC K15M resulted into highest increase in the solubility as compared to the other evaluated hydrophilic polymers. Conclusion: From the present study, we can concluded that the optimized Apixaban solid dispersion may prove to be a suitable potential option for solubility enhancement, increased in-vitro drug release and effective delivery of BCS class II and IV drugs.