Design, preparation, and evaluation of liposomal gel formulations for treatment of acne: in vitro and in vivo studies

Abstract

The study highlights the significance of co-application of bioactive components into liposomal gel formulations and their comparison to azithromycin for treatment of Acne. A Design of Experiments (DoE) approach was utilized to obtain optimized liposomal formulation encapsulating curcumin, with size and zeta potential of ∼100 nm and ∼14 mV, respectively, characterized by DLS, HR-TEM, FESEM, and AFM. The curcumin liposomal dispersion depicted excellent stability over the period of 60 days, which was further converted in gel form using Carbopol. Pharmacokinetics of curcumin-loaded liposomal gel showed that T_max for curcumin was achieved within 1 h of post application in both stratum corneum and skin, indicating quick penetration of nano-sized liposomes. Stratum corneum depicted C_max of 688.3 ng/mL and AUC_0-t of 5857.5 h × ng/mL, while the skin samples displayed C_max of 203.3 ng/gm and AUC_0-t of 2938.1 h × ng/gm. Lauric acid and azithromycin liposomal gel formulations were prepared as per the optimum parameters obtained by DoE. In antibacterial activity using agar diffusion assay, lauric acid gel formulation revealed ∼1.5 fold improved antibacterial effect than curcumin gel formulation. Interestingly, their co-application (1:1) exhibited significantly enhanced antibacterial effect against both macrolide-sensitive (1.81 versus 1.25 folds) and resistant strains of P. acnes (2.93 versus 1.22 folds) than their individual counterparts. The in vivo studies in rat ear model displayed a ∼2 fold reduction in comedones count and cytokines (TNF-α and IL-1β) on co-application with curcumin and lauric acid liposomal gel compared to placebo treated group.

Graphical Abstract

Keywords:

• Curcumin
• lauric acid
• Carbopol
• liposomes
• Propionibacterium acnes

Acknowledgments

The authors would like to acknowledge the support and contribution of Department of Drug Safety and evaluation, Sun Pharmaceutical Industries Limited, India and the Department of Microbiology of Daiichi Sankyo India Pharma Private Limited for conducting the in vivo experiments.

Disclosure statement

The authors declare no conflict of interest. This research did not receive any specific grant from funding agencies in the public, commercial, or not-for-profit sectors.