Benefits of cetalkonium chloride cationic oil-in-water nanoemulsions for topical ophthalmic drug delivery

J Pharm Pharmacol. 2014 Apr;66(4):531-41. doi: 10.1111/jphp.12075.

Abstract

Objectives: Topical ocular administration is the most convenient route of administration of drugs for the treatment of eye diseases. However, the bioavailability of drugs following eye instillations of eye drops is very low. Over the past 20 years, extensive efforts have been put into research to improve drug bioavailability without compromising treatment compliance and patients' quality of life.

Key findings: One of the most efficient ways to improve drug bioavailability is to increase the precorneal residence time of the eye drop formulations. As a result, new eye drops, with bioadhesive properties, have been developed based on the cationic oil-in-water (o/w) nanoemulsion technology. These low viscosity eye drop nanoemulsions have improved precorneal residence time through the electrostatic interactions between the positively charged oil nanodroplets and the negatively charged ocular surface epithelium.

Summary: This review is the first to present the benefits of this new strategy used to improve ocular drug bioavailability. The roles of the cationic agent in the stabilization of a safe cationic o/w nanoemulsion have been discussed, as well as the unexpected benefits of the cationic o/w nanoemulsion for the protection and restoration of a healthy tear film and corneal epithelium.

Publication types

  • Review

MeSH terms

  • Administration, Topical
  • Biological Availability
  • Cations / administration & dosage*
  • Cations / chemistry
  • Drug Delivery Systems / methods
  • Emulsions / administration & dosage*
  • Emulsions / chemistry
  • Eye Diseases / drug therapy
  • Fatty Alcohols / administration & dosage*
  • Fatty Alcohols / chemistry
  • Humans
  • Oils / administration & dosage*
  • Oils / chemistry
  • Ophthalmic Solutions / administration & dosage
  • Ophthalmic Solutions / chemistry
  • Quaternary Ammonium Compounds / administration & dosage*
  • Quaternary Ammonium Compounds / chemistry
  • Water / administration & dosage*
  • Water / chemistry

Substances

  • Cations
  • Emulsions
  • Fatty Alcohols
  • Oils
  • Ophthalmic Solutions
  • Quaternary Ammonium Compounds
  • Water
  • cetalkonium chloride