Mixed Micellization of drug-excipients and its application to enhance the binding and encapsulation efficacy of ibuprofen in aqueous media

Abstract

Drug–excipients interactions would have to be identified to increase the solubility of poorly water-soluble drugs and design better pharmaceutical formulations. This study focused on the use of chlorpheniramine maleate (CPM), an amphiphilic antihistamine drug, to optimise the encapsulation and binding of poorly water-soluble ibuprofen (IBF) in the aqueous medium. CPM was also utilised to make mixed micelles using sodium dodecyl sulphate (SDS) and sodium dioctyl sulfosuccinate (AOT). The mixed micelles of CPM-AOT and CPM-SDS revealed that CPM and AOT/SDS have a strong synergistic interaction. The objective of the mixed micelle formulation was to improve IBF binding (LogKb) and encapsulation efficiency (EE %) by increasing the αCPM 0.0–1.0 in the aqueous medium. At very high mole fraction αCPM 0.99, the maximum LogKb was 3.7 and 2.87, and the EE% was 87.08% and 78.96%, respectively. Furthermore, the molecular docking study was used to predict the position of IBF in micelles and mixed micelles, as well as its interactive features. According to the docking results, the IBF was more bind in the CPM-AOT mixture than in the CPM-SDS mixture due to electrostatic interaction. Finally, amphiphilic drugs could be employed to reduce the overuse of excipients like AOT and SDS in medicine formulation.