Abstract

AbstractThe aim of the present study was to formulate and assess the antibacterial efficacy of a transdermal chitosan based polymeric hydrogel for transdermal treatment of bacterial resistance strains. Utilizing the micro‐emulsion method and the Box–Behnken design model, imipenem‐cilastatin (IMI‐CIL) loaded nanostructured lipid carriers (NLCs) were fabricated and optimized, employing Compritol 888 ATO as the lipid core and Tween 80 as the stabilizer. The optimized nanoformulation underwent a comprehensive evaluation encompassing parameters such as particle diameter, zeta potential, surface morphology, entrapment efficiency, crystallinity, and molecular interaction. The optimized nanoparticles displayed a mean particle size of 129 nm, a zeta potential of −19.8 mV, and a polydispersity index (PDI) of 0.286. Detailed investigations into crystallinity and Fourier transform infrared (FTIR) analysis did not reveal any indications of molecular interaction. Both the IMI‐CIL loaded NLCs and the hydrogel exhibited sustained in‐vitro drug release. Moreover, the hydrogel, enriched with permeation enhancers, demonstrated a remarkable 15.77‐fold increase in drug permeation. Furthermore, the IMI‐CIL loaded NLCs exhibited significantly elevated antibacterial activity when juxtaposed with IMI‐CIL solution, which demonstrated minimal activity against non‐resistant bacterial species and lacked activity against resistant isolates. In summary, the IMI‐CIL loaded NLCs hydrogel formulation assumes a pivotal role in bestowing sustained drug release and augmenting the antibacterial efficacy of carbapenem antibiotics. This holds promise as a potential solution to combat drug‐resistant bacterial infections.

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