Utilization of amphiphilic antihistamines drugs to enhance micellization of anionic surfactant and improve the binding and solubility of Itraconazole drug

Many salt-based medicines are used in pharmaceutical formulations as active components. Excipients performance can be improved by using these medicines. The use of amphiphilic antihistamine medications (diphenhydramine hydrochloride (DPC) and cetirizine hydrochloride (CTZ)) to improve sodium dodecylbenzene sulfonate (SDBS) micellization is demonstrated in this work. DPC/CTZ considerably lowered the critical micelle concentration (CMC) of SDBS in aqueous media by measuring conductivity. SDBS micelles demonstrated a greater electrostatic interaction with CTZ than DPC micelles, based on counterion binding (beta(c) and B) and binding constant (K-b) values. The DPC/CTZ mean ion occupancy (i(0)) per SDBS micelle was also calculated using the UV spectroscopy experiment. For SDBS micelles, we observed that DPC and CTZ had i(0) values of 1.700 and 2.622, respectively. The electrostatic interaction between the medication and the surfactants was shown to be controlling the i(0) levels. The medicine Itraconazole (ITZ), which is poorly water-soluble, was found to be more soluble in SDBS micelles containing CTZ than in DPC combinations. At 0.002 mol L-1 in the aqueous medium, the greatest i(0) values of ITZ were 185 in SDBS + DPC and 203 in SDBS + CTZ. The CMC and the binding behaviour of drug-micelles were found to be critical determinants in controlling ITZ drug solubilization. Finally, we concluded that the above formulation might be used in the pharmaceutical industry to improve multi-drug delivery systems. (C) 2021 Elsevier B.V. All rights reserved.

Automated summary

This study demonstrates the improvement of sodium dodecylbenzene sulfonate (SDBS) micellization by using amphiphilic antihistamine medications (diphenhydramine hydrochloride (DPC) and cetirizine hydrochloride (CTZ)). The critical micelle concentration (CMC) of SDBS in aqueous media was significantly lowered by DPC/CTZ. The electrostatic interaction between the medication and the surfactants was found to control the ion occupancy and drug solubilization, suggesting the potential application of this formulation in multi-drug delivery systems in the pharmaceutical industry.