Development of Vancomycin, a Glycopeptide Antibiotic, in a Suitable Nanoform for Oral Delivery

Bacterial infections caused by resistant strains have emerged as one of the most significant life-threatening challenges. Developing alternatives to conventional antibiotic formulations is crucial to overcoming these challenges. Vancomycin HCl (VCM) is a glycopeptide antibiotic used for Gram-positive bacterial infections that must be given intravenously for systemic infections since it cannot pass through the gut wall due to its chemical structure and characteristics. The aim of this research is to develop VCM in a niosomal nanoform to then be encapsulated in fast-disintegrating oral films for effective delivery to enhance the application of vancomycin-loaded niosomes for treating oral infections and to be used in dental treatments. The formulation of niosomes encapsulating VCM was conducted with various ratios of Span 40, Span 60, and cholesterol as well as Kolliphor RH40 and Kolliphor ELP as co-surfactants using the microfluidic technique. The prepared niosomes were characterised using dynamic light scattering (DLS) for their size determination; high-pressure liquid chromatography, HPLC, for drug encapsulation efficiency determination; and the agar diffusion method for the determination of the antibacterial efficacy of the VCM niosomes against Bacillus subtilis. The niosomal formulation was then incorporated into polyvinyl alcohol (PVA) film, and the properties of the oral film were characterised by in vitro assays. The vancomycin-loaded niosomes produced with optimal conditions exhibited small diameter with acceptable polydispersity index, and drug encapsulation efficiency. This study presents multifunctional niosomes loaded with VCM, which demonstrated efficient in vitro activity against Gram-positive bacteria upon the slow release of VCM from niosomes, as demonstrated by the dissolution test. Oral films containing VCM niosomes demonstrated uniform weights and excellent flexibility with high foldability and a rapid disintegration time of 105 ± 12 s to release the niosomal content. This study showed that the microfluidic approach could encapsulate VCM, a peptide in salt form, in surfactant-based niosomal vesicles with a narrow size distribution. The incorporation of niosomes into fast-disintegrating film provides a non-invasive and patient-friendly alternative for treating bacterial infections in the oral cavity, making it a promising approach for dental and systemic applications.