Linezolid Loaded Nanoparticle for Topical Administration of Diabetic Foot Treatment: Formulation, In Vitro and Ex Vivo Characterization

Abstract

The aim of this research work was to develop a topical gel formulation containing nanoparticle to diabetic foot ulcer (DFU). In this respect, the nanoparticle formulations were prepared by using spontaneous emulsification technique. The linezolid (LZD) loaded nanoparticle formulation exhibited an low average particle size (PS) of 195.27±5.42 nm, low polydispersity index (PI) of 0.214±0.019, a high zeta potential (ZP) of 20.57±0.35 and high drug entrapment efficiency (EE) of 99.746±0.021%. In order to enhance topical residence time, the LZD-loaded nanoparticles were dispersed in a gel formulation using Methocel TM K4M (HPMC) and Carbopol® 974 P NF. The formulated gels demonstrated favorable characteristics, including an appropriate pH value, suitable mechanical performance, and desirable viscosity and spreadability for topical administration. All formulations displayed pseudoplastic flow and exhibited typical gel-type mechanical spectra at the specified frequency value. Moreover, the developed formulation achieved sustained drug release as intended for these systems. During the ex vivo drug diffusion studies, 0.007±0.004% of LZD was found in receptor phase, and this was an indicator of local effect. The optimum formulation was stable for 6 months. The initial findings suggest that the formulated topical gel containing LZD-loaded nanoparticles holds promise as an effective drug delivery system for DFU management. However, further comprehensive investigations are required to substantiate this hypothesis.