Pharmacosomes encapsulated with Dapsone and Cloxacilline to Enhance Transdermal Penetration: In Vitro and Ex Vivo Study

Abstract

This work is based on to evaluate pharmacosome-based topical gel formulations for enhanced transdermal supply of Dapsone (DAP) and Cloxacillin (CLXS). Drug-excipient compatibility was confirmed by FTIR, indicating no any type of interaction. pharmacosomes (P1–P9) were categorized for vesicle size (110.6–168.2 nm), zeta potential (–14.7 to –30.5 mV), and high encapsulation efficiency (%EE), with optimized formulations (P4–P6) showing greater physicochemical properties. Among these, P5 exhibited optimal discharge behavior and smallest vesicle size. Pharmacosomal gels (G1–G9) were formulated using Carbopol 934 and calculated for drug content, spreadability, pH, and viscosity. Optimized gel G5 confirmed high drug content (83.54%), suitable pH (6.8), and ideal spreadability. In-vitro and ex-vivo studies show sustained drug release (up to 85.36 % over 24 h) and increased skin permeation compared to other conventional gels. TEM and SEM analyses show spherical morphology with even vesicle distribution. Stability studies over three months presented no major changes in vesicle characteristics, approving the formulation are stable. The presence of PEG 400 and low Carbopol concentration in G5 enhanced vesicle flexibility and skin permeation. Overall, the pharmacosomal gel (G5) show a stable vasicular delivery, active transdermal delivery system for enhanced topical delivery of DAP and CLXS.  This vesicular gel was ready by using different optimization parameters. By comparing all the gel formulations, we observe that the vesicular gel exhibits the best drug release. In summary, the existence of DAP and CLXS in pharmacosomes is capable to enhance the anti-leprotic preparation, and it provide the cumulative effect on the patients.