Loading Of Gentamicin And Alpha Lipoic Acid On A Biodegradable Polymer For More Effective And Less Nephrotoxic Formula

Background and Objective: Gentamicin sulphate (GN) is a broad-spectrum antibiotic used for treatment of several types of infection. However, it can cause vasoconstriction, leading to serious ad verse effects, such as kidney damage and inner ear problems. The aim of this study was to suppress GN nephrotoxicity and to sustain its release. Methodology: Polycaprolactone (PCL) nanoparticles (NPs) were loaded with GN and alpha lipoic acid (ALA) using the solvent evaporation technique. The prepared NPs were assessed for particle size, zeta potential, morphology, entrapment efficiency percentage and GN release. Finally, an in vivo nephrotoxicity study was carried out to assess the protective effect of ALA on the kidneys of rabbits. Results: Data revealed that the prepared GN-ALA-PCL NPs were in the nano size range. GN was released more slowly than pure GN, thus sustaining its effect. Creatinine increased 1.4-fold in the pure GN group in comparison with the control group and other electrolytes (sodium, calcium and potassium) showed abnormal results for the pure GN group. There was no significant difference in creatinine and the other electrolytes between the GN-ALA-PCL NPs group and the control group. Data confirm the protective effect of ALA against GN nephrotoxicity. Conclusion: Loading of GN with ALA on PCL NPs could be a successful strategy to inhibit GN nephrotoxicity and extend GN release, which enhances its safety and dose frequency profiles.