Moxifloxacin loaded gelatin nanoparticles for ocular delivery: Formulation and in-vitro, in-vivo evaluation

J Colloid Interface Sci. 2016 Dec 1:483:132-138. doi: 10.1016/j.jcis.2016.08.018. Epub 2016 Aug 10.

Abstract

The current research focuses on developing positively charged gelatin nanoparticles loaded with moxifloxacin for its effective ocular delivery and controlled release in corneal eye layer. We selected type A gelatin because of its biodegradable and non-toxic nature as the polymer of choice for fabricating the nanoparticles by a modified two step desolvation technique. The produced nanoparticles were positively charged (+24±0.12mV) with a narrow particle size of 175±1.11nm as measured by dynamic light scattering (DLS). The in-vitro drug release from the nanoformulations exhibited a burst effect in the first hour followed by a controlled release of the drug for the subsequent 12h. The Korsmeyer-Peppas model showed better linearity and the formulations displayed non-Fickian drug release pattern. The optimized formulation was assessed for its utility as an anti-bacterial agent and its effectiveness was tested on the corneal eye surface of rabbits. The in-vivo tolerance tests revealed that the drug loaded nano-formulations was non-irritant to the ocular tissues indicating its safety. The in-vivo anti-bacterial activity of the nanosuspension was more effective against S. aureus than the commercially market product, MoxiGram®. Microbiological efficacy assessed against B. subtilus using cup-plate method suggested that our fabricated nanosuspension possess better anti-microbial activity as compared to the commercial agent, MoxiGram® revealing promising potentials for the currently developed gelatin based nanoformualtions.

Keywords: Bacillus subtilus; Gelatin; In-vivo tolerance; Moxifloxacin; Ocular tissues; Staphylococcus aureus.

MeSH terms

  • Administration, Ophthalmic
  • Animals
  • Anti-Bacterial Agents / pharmacokinetics*
  • Anti-Bacterial Agents / pharmacology
  • Bacillus subtilis / drug effects
  • Bacillus subtilis / growth & development
  • Cornea / drug effects*
  • Cornea / metabolism
  • Cornea / microbiology
  • Delayed-Action Preparations*
  • Disk Diffusion Antimicrobial Tests
  • Drug Compounding
  • Drug Liberation
  • Drug Stability
  • Fluoroquinolones / pharmacokinetics*
  • Fluoroquinolones / pharmacology
  • Gelatin / chemistry*
  • Male
  • Moxifloxacin
  • Nanoparticles / chemistry*
  • Nanoparticles / ultrastructure
  • Particle Size
  • Rabbits
  • Solubility
  • Staphylococcus aureus / drug effects
  • Staphylococcus aureus / growth & development
  • Static Electricity

Substances

  • Anti-Bacterial Agents
  • Delayed-Action Preparations
  • Fluoroquinolones
  • Gelatin
  • Moxifloxacin