Nanoemulsion as a feasible and biocompatible carrier for ocular delivery of travoprost: Improved pharmacokinetic/pharmacodynamic properties

Int J Pharm. 2020 Jun 15;583:119402. doi: 10.1016/j.ijpharm.2020.119402. Epub 2020 May 5.

Abstract

Travoprost is a synthetic prostaglandin F2α analogue used in treatment of glaucoma. Due to its water insolubility and oily nature, novel delivery systems need to be developed to enhance its bioavailability, and sustain its release. In the current work, travoprost nanoemulsion was explored as a novel carrier prepared using low energy technique. Results showed that travoprost nanoemulsions exhibited suitable nanodroplet size, zeta potential, pH, refractive index, controlled release, as well as sufficient stability under accelerated conditions. In vivo studies delineated the enhanced absorption of travoprost nanoemulsion compared to the marketed eye drops Travatan®, as proven by the higher Cmax and AUC of the former, and its prolonged intraocular pressure reduction time. Moreover, the nanoemulsion formulation was proven safe and non-irritant to ocular surfaces. Therefore, it can be suggested that travoprost nanoemulsion is a promising ocular delivery system for glaucoma treatment.

Keywords: Glaucoma; Nanoemulsion; Pharmacokinetics; Stability; Travoprost.

Publication types

  • Comparative Study

MeSH terms

  • Administration, Ophthalmic
  • Animals
  • Antihypertensive Agents / administration & dosage*
  • Antihypertensive Agents / pharmacokinetics*
  • Antihypertensive Agents / toxicity
  • Biological Availability
  • Drug Carriers*
  • Drug Compounding
  • Emulsions
  • Feasibility Studies
  • Glaucoma / drug therapy
  • Glaucoma / physiopathology
  • Intraocular Pressure / drug effects
  • Lipids / chemistry*
  • Nanoparticles*
  • Ocular Absorption
  • Ophthalmic Solutions
  • Rabbits
  • Travoprost / administration & dosage*
  • Travoprost / pharmacokinetics*
  • Travoprost / toxicity

Substances

  • Antihypertensive Agents
  • Drug Carriers
  • Emulsions
  • Lipids
  • Ophthalmic Solutions
  • Travoprost