Formulation and Evaluation of Imiquimod-Loaded Ethosomal Gel for Enhanced Topical Therapy of Skin Cancer

Abstract

Imiquimod doesn't dissolve or permeate the skin efficiently, limiting its topical application and causing localized discomfort and poor response. In ethosomal vesicles, imiquimod is easier to penetrate the skin, stays in the skin longer, is less toxic, and is more effective against skin cancer, particularly melanoma. A modified cold approach was used to make imiquimod ethosomal formulations.  Using Box-Behnken Design, we optimized phospholipid, ethanol, and propylene glycol concentrations. The improved formulations' vesicle size, entrapment efficiency, flux, TEM, DSC, XRD, and chemical compatibility were examined.  In vitro experiments included apoptosis (DAPI, flow cytometry), DNA fragmentation, colony formation assays, A375 melanoma and L929 fibroblast cell uptake and cytotoxicity, and Franz diffusion cell skin penetration.  The gel's stability, histology, skin adhesion, and physicochemical characteristics were examined after mixing an improved ethosomal formulation (IMQ-ETH) with a carbopol gel.  Improved ethosomal gel (IMQ-ETH) showed 87.47% entrapment efficacy, nanosized spherical vesicles (100 nm), and five times greater epidermal penetration than standard gel.  The medicine penetrated deep into the skin and killed melanoma cells by boosting apoptosis and nuclear absorption, according to fluorescence imaging and in vitro experiments.  The formulation improved Imiquimod's localized distribution and therapeutic efficacy, making it a potent topical skin cancer rival.