Noninvasive biodegradable nanoparticles-in-nanofibers single-dose ocular insert: in vitro, ex vivo and in vivo evaluation

Nanomedicine (Lond). 2019 Jan;14(1):33-55. doi: 10.2217/nnm-2018-0297. Epub 2018 Dec 13.

Abstract

Aim: This study involves, for the first time, the development of mucoadhesive biodegradable polymeric-multilayered nanoparticles-in-nanofibers (NPs-in-NFs) matrix as an innovative single-dose noninvasive ocular-insert that could substitute conventional ocular dosage-forms.

Materials & methods: Azithromycin-loaded poly(lactic-co-glycolic acid) copolymer/pluronic NPs were developed then incorporated into electrospun polyvinylpyrrolidone NFs, and tested for their efficient treatment of ocular bacterial infection.

Results: Release and permeation studies proved the ability of the insert to control drug release over 10 days.

Conclusion: The incorporation of NPs into NFs achieved several other benefits like increasing ocular residence and contact time with conjunctival tissue, accurate dose delivery, sustaining drug release with constant rate, reducing frequency of administration, improving bioavailability along with decreasing incidence of visual and systemic side effects.

Keywords: azithromycin; bacterial infection; electrospun; nanofibers; ocular; single-dose.

Publication types

  • Evaluation Study

MeSH terms

  • Animals
  • Anti-Bacterial Agents / administration & dosage
  • Anti-Bacterial Agents / pharmacokinetics
  • Azithromycin / administration & dosage
  • Azithromycin / adverse effects
  • Azithromycin / pharmacokinetics*
  • Biological Availability
  • Cell Line
  • Cell Survival / drug effects
  • Delayed-Action Preparations / chemistry
  • Drug Carriers / chemistry*
  • Drug Carriers / pharmacokinetics
  • Drug Liberation
  • Eye / metabolism*
  • Humans
  • Nanofibers / chemistry*
  • Nanoparticles / chemistry*
  • Particle Size
  • Polylactic Acid-Polyglycolic Acid Copolymer / chemistry*
  • Rabbits
  • Surface Properties

Substances

  • Anti-Bacterial Agents
  • Delayed-Action Preparations
  • Drug Carriers
  • Polylactic Acid-Polyglycolic Acid Copolymer
  • Azithromycin