In vitro and in vivo evaluation of tedizolid nanoparticle incorporated buccal films for oromucosal infections

Int J Pharm. 2024 Nov 15:665:124688. doi: 10.1016/j.ijpharm.2024.124688. Epub 2024 Sep 16.

Abstract

A novel tedizolid phosphate (TZP) nanoparticle (NP)-loaded buccal film formulation was developed for the treatment of buccal wounds infected with S. aureus. TZP-loaded chitosan NPs were produced and characterized to prepare this composite system. The optimum NP formulation was then loaded into mucoadhesive buccal films. The antibacterial effects of the obtained buccal films were evaluated by in vitro and in vivo studies. The optimum TZP-NP formulation (F8) had a particle size of 177.40 ± 2.97 nm and PDI and ZP values were 0.437 ± 0.002 and 33.9 ± 0.5, respectively. In antibacterial efficacy tests, the optimum NP containing buccal film formulation was used, which released approximately 90 % of TZP within 5 h. TZP-NP-loaded buccal films achieved a 3 log10 reduction in S. aureus within just 3 h. It was also administered to Wistar albino rats with S. aureus-infected buccal wounds. As a result of in vivo studies, a significant decrease in the number of S. aureus was detected in wound samples treated with TZP-NP-loaded buccal films. In addition, a complete inhibition of growth was observed on the fifth day of the film application. The current work suggested that the TZP-NP-loaded composite films could be promising candidates for effective and long-acting antibacterial treatment of buccal wounds.

Keywords: Antibacterial efficacy; Buccal film; Mucoadhesive film; Nanoparticle; Tedizolid phosphate.

MeSH terms

  • Administration, Buccal
  • Animals
  • Anti-Bacterial Agents* / administration & dosage
  • Anti-Bacterial Agents* / chemistry
  • Anti-Bacterial Agents* / pharmacology
  • Chitosan / administration & dosage
  • Chitosan / chemistry
  • Drug Liberation
  • Male
  • Mouth Mucosa / drug effects
  • Mouth Mucosa / microbiology
  • Nanoparticles* / chemistry
  • Organophosphates / administration & dosage
  • Organophosphates / chemistry
  • Organophosphates / pharmacology
  • Oxazoles / administration & dosage
  • Oxazoles / chemistry
  • Oxazolidinones / administration & dosage
  • Oxazolidinones / chemistry
  • Particle Size
  • Rats
  • Rats, Wistar*
  • Staphylococcal Infections* / drug therapy
  • Staphylococcus aureus* / drug effects
  • Tetrazoles

Substances

  • Anti-Bacterial Agents
  • Oxazoles
  • Chitosan
  • tedizolid phosphate
  • Organophosphates
  • Oxazolidinones
  • tedizolid
  • Tetrazoles