Chitosan as tear substitute: a wetting agent endowed with antimicrobial efficacy

J Ocul Pharmacol Ther. 2000 Jun;16(3):261-70. doi: 10.1089/jop.2000.16.261.

Abstract

A cationic biopolymer, chitosan, is proposed for use in artificial tear formulations. It is endowed with good wetting properties as well as an antibacterial effect that are desirable in cases of dry eye, which is often complicated by secondary infections. Solutions containing 0.5% w/v of a low molecular weight (M(w)) chitosan (160 kDa) were assessed for antibacterial efficacy against E. coli and S. aureus by using the usual broth-dilution technique. The in vitro evaluation showed that concentrations of chitosan as low as 0.0375% still exert a bacteriostatic effect against E. coli. Minimal inhibitory concentration (MIC) values of chitosan were calculated to be as low as 0.375 mg/ml for E. coli and 0.15 mg/ml for S. aureus. Gamma scintigraphic studies demonstrated that chitosan formulations remain on the precorneal surface as long as commonly used commercial artificial tears (Protagent collyrium and Protagent-SE unit-dose) having a 5-fold higher viscosity.

MeSH terms

  • Animals
  • Anti-Bacterial Agents / pharmacokinetics
  • Anti-Bacterial Agents / pharmacology*
  • Biopolymers / pharmacokinetics
  • Biopolymers / pharmacology
  • Chitin / analogs & derivatives
  • Chitin / pharmacokinetics
  • Chitin / pharmacology*
  • Chitosan
  • Cornea / metabolism
  • Escherichia coli / drug effects*
  • Male
  • Microbial Sensitivity Tests
  • Ophthalmic Solutions / pharmacokinetics
  • Ophthalmic Solutions / pharmacology*
  • Rabbits
  • Staphylococcus aureus / drug effects*
  • Viscosity
  • Wettability

Substances

  • Anti-Bacterial Agents
  • Biopolymers
  • Ophthalmic Solutions
  • Chitin
  • Chitosan