Vancomycin Hydrochloride

Vancomycin hydrochloride is a glycopeptide antibiotic that exerts its bactericidal activity through a specific and high-affinity interaction with the bacterial cell wall precursor. The primary mechanism involves the formation of a complex network of hydrogen bonds and hydrophobic interactions with the D-Ala-D-Ala terminus of the Lipid II molecule, which is a key component in the synthesis of the bacterial cell wall. This binding effectively prevents the cross-linking of peptidoglycan strands by blocking the action of essential enzymes, such as transglycosylases and transpeptidases. As a result, the bacteria are unable to synthesize a complete and functional cell wall, which compromises their structural integrity. This disruption makes the cells susceptible to osmotic pressure, ultimately leading to cell lysis and death. While inhibition of cell wall synthesis is the primary action, some studies suggest that vancomycin may also have secondary effects on bacterial RNA synthesis.

Fig. 1 Mechanism of vancomycin action. (Tabarzad M.; et al. 2025)

Vancomycin hydrochloride was successfully formulated into polymeric microarray patches for transdermal delivery, overcoming the poor oral bioavailability of this peptide antibiotic. Two types of patches were developed: dissolving microarray patches and hydrogel-forming microarray patches. Both systems achieved significant transdermal permeation in ex vivo studies using neonatal porcine skin. In vivo pharmacokinetic studies in rats demonstrated that hydrogel-forming microarray patches achieved an area under the plasma concentration-time curve of 162.04 μg·h/mL, significantly higher than oral administration controls. This work demonstrated that transdermal delivery of vancomycin hydrochloride via microarray patches is feasible and could provide an effective alternative to intravenous administration for treating MRSA infections, particularly for skin and soft tissue infections.

Fig. 2 Preparation and characterization of Vancomycin hydrochloride-based polymeric microarray patches. (Ramadon D.; et al. 2020)