Development of Oral Gentamicin Nanoparticles for Enhanced Intestinal Permeability and Bioavailability

Abstract

Gentamicin is a really effective aminoglycoside antibiotic that’s often used for serious Gram-negative infections. Still, it doesn’t absorb well when taken by mouth, and because it usually needs intravenous administration, it ends up being less friendly for outpatient use and also drives higher healthcare costs. This study was meant to sort of craft a nanoparticle-based oral formulation that could raise gentamicin absorption and its overall bioavailability.

Two separate nanoparticle setups were prepared to hold gentamicin inside: solid lipid nanoparticles, also called SLNs, and PLGA /chitosan polymeric nanoparticles. The idea behind both systems was pretty similar; they were built to shield gentamicin from gastrointestinal breakdown and to help it cross the mucosal barrier more easily. The formulations were then checked for particle size, zeta potential, encapsulation efficiency, and basic in vitro drug release behavior. After that, ex vivo permeability experiments were done with rat jejunal tissue, so we could get a sense of how well the drug is transported across the intestine.

Then, in vivo pharmacokinetic work was carried out in rodents, measuring gentamicin levels in plasma after oral dosing with the nanoparticle formulations. The preliminary results showed that the nanoparticle versions noticeably boosted intestinal uptake, and they generated detectable systemic drug concentrations, unlike unformulated gentamicin. Overall, these observations lend support to the proof of concept for changing intravenous gentamicin into a possible oral therapy. If this direction keeps working out, it may improve patient adherence, lower the need for hospital stays, and widen treatment access.

Future studies should emphasize dose optimization, longer-term safety assessments, and scaling up the formulation process for potential clinical use.