In-situ forming gels containing fluorometholone-loaded polymeric nanoparticles for ocular inflammatory conditions

Colloids Surf B Biointerfaces. 2019 Mar 1:175:365-374. doi: 10.1016/j.colsurfb.2018.11.065. Epub 2018 Nov 27.

Abstract

Thermosensitive gels have been developed and optimized in such a way that they become gels at corneal temperature and with a viscosity that allows the adequate release of the Fluorometholone (FMT)-loaded PLGA nanoparticles (NPs) in order to improve ocular anti-inflammatory efficacy against a commercial formulation. It has been shown that gels avoid burst release of the drug in the first hours with a slow and increasing profile after administration. NPs have maintained their average size and spherical shape within the gels as confirmed by transmission electron microscopy (TEM). In turn, the in-situ gelling of the formulations allows the administration in eye drops dosage form due to its state of sol at temperatures below 25 °C. Ocular tolerance studies have shown that no formulation causes eye irritation. The administration of the developed formulations has improved the precorneal residence time reflected in the ocular bioavailability, where deep tissues as aqueous humour and crystalline were reached. In conclusion, the use of thermosensitive gels for the topical application of NPs has demonstrated their effectiveness in the acute and preventive treatment of ocular inflammatory conditions.

Keywords: Fluorometholone; Gel; In-situ gelling; Ocular anti-inflammatory; PLGA nanoparticles; Poloxamer 407; Thermosensitive.

MeSH terms

  • Administration, Ophthalmic
  • Animals
  • Anti-Inflammatory Agents / administration & dosage*
  • Anti-Inflammatory Agents / chemistry
  • Biological Availability
  • Drug Delivery Systems*
  • Eye Diseases / drug therapy*
  • Fluorometholone / chemistry*
  • Gels / chemistry*
  • Male
  • Nanoparticles / administration & dosage*
  • Nanoparticles / chemistry
  • Polymers / chemistry*
  • Rabbits

Substances

  • Anti-Inflammatory Agents
  • Gels
  • Polymers
  • Fluorometholone