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

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 (LogK(b)) and encapsulation efficiency (EE %) by increasing the alpha(CPM) 0.0-1.0 in the aqueous medium. At very high mole fraction alpha(CPM) 0.99, the maximum LogK(b) 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.

Automated summary

This study focused on using the amphiphilic drug CPM to optimize the encapsulation and binding of poorly water-soluble IBF, as well as to make mixed micelles. The results showed that increasing the alpha value of CPM can improve drug binding and encapsulation efficiency. Molecular docking study indicated that IBF binds more easily in the CPM-AOT mixture due to electrostatic interaction.