Preparation and in vivo evaluation of in situ gel system as dual thermo-/pH-responsive nanocarriers for sustained ocular drug delivery

J Microencapsul. 2015;32(5):511-9. doi: 10.3109/02652048.2015.1065915. Epub 2015 Jul 20.

Abstract

Objective: Ciprofloxacin (CIP) was effective in treating bacterial keratitis. The purpose of this study was to prepare an effective prolonged-release of CIP by both temperature and pH-triggered in situ nanogels for the treatment of keratitis.

Materials and methods: Poly(N-isopropylacrylamide-methacrylicacide-vinylpyrrolidone) [P (NIPAAm-MAA-VP)] nanoparticles was synthesised and used for preparation of CIP-loaded nanogels. Antimicrobial and in vivo animal studies of the CIP-loaded nanoformulation were performed.

Results: Nanoformulation with a mean particle size between 10 and 50 nm and higher than 95% encapsulation efficiency was obtained. Ciprofloxacin released from the nanoparticles showed an enhanced antibacterial effect as determined by minimal inhibitory concentrations. In vivo studies demonstrated reasonable efficacy in severe keratitis using the developed nanoformulation.

Conclusions: Nanoformulation had acceptable efficacy in treating bacterial keratitis in an animal model. Therefore, the developed system has the potential to be used in localised application for the treatment of keratitis.

Keywords: In situ nanogel; antimicrobial activity; ciprofloxacin; dual stimuli responsive; keratitis; ocular drug delivery.

MeSH terms

  • Administration, Ophthalmic
  • Anti-Bacterial Agents* / chemistry
  • Anti-Bacterial Agents* / pharmacokinetics
  • Anti-Bacterial Agents* / pharmacology
  • Ciprofloxacin* / chemistry
  • Ciprofloxacin* / pharmacokinetics
  • Ciprofloxacin* / pharmacology
  • Drug Carriers* / chemistry
  • Drug Carriers* / pharmacokinetics
  • Drug Carriers* / pharmacology
  • Gels / chemistry
  • Gels / pharmacokinetics
  • Gels / pharmacology
  • Humans
  • Keratitis / drug therapy
  • Methacrylates* / chemistry
  • Methacrylates* / pharmacokinetics
  • Methacrylates* / pharmacology
  • Nanoparticles / chemistry*
  • Particle Size

Substances

  • Anti-Bacterial Agents
  • Drug Carriers
  • Gels
  • Methacrylates
  • Ciprofloxacin