Nanostructured lipid carriers-based thermosensitive eye drops for enhanced, sustained delivery of dexamethasone

Nanomedicine (Lond). 2018 Jun;13(11):1239-1253. doi: 10.2217/nnm-2017-0318.

Abstract

Aim: Nanostructured lipid carriers in-gel (NLCs-gel) were prepared to enhance and improve the ocular delivery of dexamethasone. Materials & methods: NLCs containing dexamethasone prepared by high-pressure homogenization were characterized and dispersed into thermosensitive gels (Pluronic F127 and F68 as gels material). In vitro drug release studies, ocular irritation tests, ex vivo corneal penetration and drug dynamics of NLCs and NLCs-gel were evaluated in aqueous humor.

Results: NLCs-gel exhibited a rapid sol-gel transition at 34.4°C and presented nano-sized, narrowly distributed particles. Corneal penetration studies revealed steady sustained drug release (Ritger-Peppas); NLCs-gel increased ocular bioavailability by prolonging precorneal retention time and improving corneal permeation.

Conclusion: These findings suggest developing NLCs-gel for potential treatment of posterior segment eye diseases.

Keywords: dexamethasone; nanostructured lipid carrier; ocular bioavailability; posterior segment eye disease; thermosensitive gel.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Biological Availability
  • Chitosan / administration & dosage
  • Chitosan / chemistry
  • Cornea / drug effects
  • Cornea / pathology
  • Delayed-Action Preparations / administration & dosage
  • Delayed-Action Preparations / chemistry
  • Dexamethasone / administration & dosage*
  • Dexamethasone / chemistry
  • Drug Carriers / administration & dosage
  • Drug Carriers / chemistry
  • Drug Liberation / drug effects
  • Eye Diseases / drug therapy*
  • Humans
  • Lipids / administration & dosage
  • Lipids / chemistry
  • Nanostructures / administration & dosage*
  • Nanostructures / chemistry
  • Ophthalmic Solutions / administration & dosage*
  • Ophthalmic Solutions / chemistry
  • Rabbits

Substances

  • Delayed-Action Preparations
  • Drug Carriers
  • Lipids
  • Ophthalmic Solutions
  • Dexamethasone
  • Chitosan