Vancomycin Insights: An Update on Mechanism, Activity, Toxicity, Resistance, and Novel Drug Delivery Systems

Vancomycin is an important antibiotic with a glycopeptide structure, effective against gram-positive bacterial infections through the inhibition of bacterial cell wall biosynthesis. It is indicated for the treatment of serious complicated skin, bloodstream, lower respiratory tract, bone, and joint infections. Primarily administered intravascularly, vancomycin shows negligible oral bioavailability. This review discusses the mechanism of action and toxicity of vancomycin, along with resistance issues and the mechanisms involved.

We covered updated literature regarding various delivery systems for vancomycin, including nanoparticles, nanofibers, microparticles, liposomes, and hydrogels. Their antimicrobial evaluations and significant results are presented, alongside summaries of attempts for vancomycin oral delivery. The main issues of vancomycin, such as poor physicochemical properties (high molecular mass and aqueous solubility), poor oral bioavailability, minimum inhibitory concentration (MIC) creep, emergence of resistance, and high tendency to accumulate in the kidneys, can be addressed using novel drug delivery systems.

We summarized a range of novel drug delivery systems that have been investigated for enhancing the efficacy of vancomycin. The data collected here could be used as a guide for fabricating proper carriers for vancomycin delivery and selecting appropriate antimicrobial tests. Further in-depth studies on the mechanisms by which nanoparticles overcome resistance and enhance drug efficacy may pave the way for designing more effective systems.