title: Antinociceptive activity of Delta9-tetrahydrocannabinol non-ionic microemulsions.
abstract: Delta(9)-Tetrahydrocannabinol (Delta(9)-THC), the major psychoactive constituent of Cannabis sativa L., has been widely studied for its potential pharmaceutical application in the treatment of various diseases and disturbs. This sparingly soluble terpeno-phenolic compound is not easy to handle and to be formulated in pharmaceutical preparations. The aim of this work was to develop a stable aqueous Delta(9)-THC formulation acceptable for different ways of administration, and to evaluate the therapeutic properties of the new Delta(9)-THC based preparation for pain treatment. Due to the thermodynamic stability and advantages of microemulsion based systems, the study was focused on the identification of aqueous microemulsion based systems containing Delta(9)-THC. Oil in water Delta(9)-THC microemulsions were individuated through phase diagrams construction, using the non-ionic surfactant Solutol HS15, being this surfactant acceptable for parenteral administration in human. A selected microemulsion samples containing 0.2 wt% of Delta(9)-THC, stable up to 52 degrees C, was successfully assayed on animal models of pain. Significant antinociceptive activity has been detected by both intraperitoneal and intragastric administration of the new Delta(9)-THC pharmaceutical preparation. The effect has been highlighted in shorter time if compared to a preparation of the same active principle based on previously reported conventional preparation.
authors.affiliation: Neuroscienze PharmaNess S.c.a r.l., c/o Sardegna Ricerche, Edificio 5, Località Piscinamanna, 09010 Pula (Cagliari), Italy. paolo.lazzari@pharmaness.it
authors.forename: P
authors.initials: P
authors.lastname: Lazzari
authors.forename: P
authors.initials: P
authors.lastname: Fadda
authors.forename: G
authors.initials: G
authors.lastname: Marchese
authors.forename: G L
authors.initials: GL
authors.lastname: Casu
authors.forename: L
authors.initials: L
authors.lastname: Pani
mesh_terms: D000284:Administration, Oral; D000700:Analgesics / Q000008:administration & dosage / Q000737:chemistry / Q000494:pharmacology*; D000818:Animals; D002626:Chemistry, Pharmaceutical; D004195:Disease Models, Animal; D013759:Dronabinol / Q000008:administration & dosage / Q000737:chemistry / Q000494:pharmacology*; D004339:Drug Compounding; D004355:Drug Stability; D004655:Emulsions; D007274:Injections, Intraperitoneal; D008297:Male; D051379:Mice; D010146:Pain / Q000503:physiopathology / Q000517:prevention & control*; D010147:Pain Measurement; D017288:Pain Threshold / Q000187:drug effects*; D011092:Polyethylene Glycols / Q000737:chemistry; D011930:Reaction Time; D012995:Solubility; D013229:Stearic Acids / Q000737:chemistry; D013501:Surface-Active Agents / Q000737:chemistry; D013678:Technology, Pharmaceutical / Q000379:methods; D013696:Temperature; D013997:Time Factors
chemical_list: D000700:Analgesics; D004655:Emulsions; D013229:Stearic Acids; D013501:Surface-Active Agents; D011092:Polyethylene Glycols; C067028:Solutol HS 15; D013759:Dronabinol