Human Immunodeficiency Virus (HIV) remains a major global health challenge despite advances in antiretroviral therapy. Etravirine, a second-generation non-nucleoside reverse transcriptase inhibitor, exhibits potent antiviral activity but suffers from poor aqueous solubility, variable oral bioavailability, and extensive first-pass metabolism. The present study aimed to develop and evaluate an Etravirine-loaded ethosomal hydrogel for transdermal delivery to overcome these limitations. Preformulation studies confirmed the lipophilic nature of the drug (log P 5.5–6.0) and its poor aqueous solubility. Ethosomes were prepared using varying compositions and evaluated for vesicle size, polydispersity index, zeta potential, entrapment efficiency, and deformability. The optimized formulation (F5) exhibited high entrapment efficiency (88.9%), good stability, and enhanced deformability. The ethosomal dispersion was incorporated into a Carbopol 940 hydrogel and evaluated for physicochemical properties. The optimized hydrogel (F5) showed suitable pH (5.5), high viscosity (12,500 cP), excellent gel strength, and uniform drug content. In-vitro drug release studies demonstrated sustained release (96.8% at 12 hours). Kinetic analysis revealed that drug release followed the Higuchi model (R² = 0.991) and Korsmeyer–Peppas mechanism (n = 0.62), indicating diffusion-controlled release with polymer relaxation. The study concludes that the developed ethosomal hydrogel system is a promising transdermal delivery platform for Etravirine, offering improved bioavailability, sustained drug release, and enhanced patient compliance.
Suresh Kumar*, Dr. Tara Chand, Ashish Jain, Priyanka, Chetan Raj Singh (Wed,) studied this question.