A submicron emulsion of HU-211, a synthetic cannabinoid, reduces intraocular pressure in rabbits

Graefes Arch Clin Exp Ophthalmol. 2000 Apr;238(4):334-8. doi: 10.1007/s004170050361.

Abstract

Purpose: To study the ocular hypotensive effect of a nonpsychotropic cannabinoid, HU-211 (11 -hydroxy-delta8-tetra-hydrocannabinol, dimethylheptyl), an N-methyl-D-aspartate (NMDA) agonist, in normotensive rabbits.

Methods: The cannabinoid HU-211, being lipophilic, was incorporated into a stable oil-in-water submicron sterile emulsion, consisting of 0.12% (w/w) HU-211. A single- dose, randomized and double-masked study was designed, using a Digilab 30R pneumotonometer to measure intraocular pressure (IOP) in normotensive rabbits.

Results: Application of a single dose of HU-211 ophthalmic preparation resulted in an IOP reduction of 5.3 mmHg (24% of baseline), first evident at 1.5 h post application and persisting for over 6 h. A small but significant lowering of pressure (12.5% of baseline) occurred in the contralateral eyes of HU-211 treated rabbits, lasting for 4 h post treatment.

Conclusion: Our work demonstrated that HU-211, incorporated into submicron emulsion, caused a 6-h-long reduction in IOP in the treated eye, with a lesser reduction in the contralateral untreated eye.

MeSH terms

  • Administration, Topical
  • Animals
  • Cannabinoids / administration & dosage
  • Cannabinoids / pharmacokinetics
  • Cannabinoids / pharmacology*
  • Cornea / metabolism
  • Dronabinol / administration & dosage
  • Dronabinol / analogs & derivatives*
  • Dronabinol / pharmacokinetics
  • Dronabinol / pharmacology*
  • Emulsions
  • Excitatory Amino Acid Antagonists / administration & dosage
  • Excitatory Amino Acid Antagonists / pharmacokinetics
  • Excitatory Amino Acid Antagonists / pharmacology*
  • Female
  • Intraocular Pressure / drug effects*
  • Male
  • Ophthalmic Solutions / administration & dosage
  • Ophthalmic Solutions / pharmacology
  • Rabbits
  • Random Allocation
  • Tonometry, Ocular

Substances

  • Cannabinoids
  • Emulsions
  • Excitatory Amino Acid Antagonists
  • Ophthalmic Solutions
  • Dronabinol
  • HU 211