Cyclosporine a-loaded solid lipid nanoparticles: ocular tolerance and in vivo drug release in rabbit eyes

Curr Eye Res. 2009 Nov;34(11):996-1003. doi: 10.3109/02713680903261405.

Abstract

Purpose: To determine the in vivo efficacy of cyclosporine A-loaded solid lipid nanoparticles (SLNs) in rabbit eyes.

Methods: SLNs were prepared and administered to the cul-de-sac of rabbits, and the drug amount in aqueous humor was detected by high performance liquid chromatography (HPLC). The irritation was evaluated by modified Draize testing.

Results: The particle size of SLNs was detected as 225.9 +/- 5.5 nm with a negative surface charge. Aqueous humor drug levels reached 50.53 ng/mL, and there was no serious irritation in rabbit eyes.

Conclusions: Topical ophthalmic efficacy of cyclosporine A was enhanced via administration of SLNs.

MeSH terms

  • Animals
  • Aqueous Humor / metabolism
  • Biological Availability
  • Biological Transport, Active
  • Chromatography, High Pressure Liquid
  • Cyclosporine / administration & dosage*
  • Cyclosporine / adverse effects
  • Cyclosporine / pharmacokinetics
  • Drug Delivery Systems*
  • Immunosuppressive Agents / administration & dosage*
  • Immunosuppressive Agents / adverse effects
  • Immunosuppressive Agents / pharmacokinetics
  • Lipids / chemistry*
  • Male
  • Nanoparticles / administration & dosage*
  • Nanoparticles / chemistry
  • Particle Size
  • Rabbits

Substances

  • Immunosuppressive Agents
  • Lipids
  • Cyclosporine