Hydroxypropyl-β-cyclodextrin and its combination with hydroxypropyl-methylcellulose increases aqueous solubility of Δ9-tetrahydrocannabinol

Delta(9)-tetrahydrocannabinol (THC) is the main psychoactive constituent of Cannabis sativa L. and its therapeutic effects are currently under intensive study. However, THC has a very low aqueous solubility (1-2 mu g/mL), which restricts its use as a pharmaceutical. The present study demonstrates that THC forms a drug-cyclodextrin complex in an aqueous solution of hydroxypropyl-beta-cyclodextrin (HP-beta-CD), resulting in a thousand-fold increase in THC solubility. This improvement in solubility can be further increased by adding 0.1% hydroxypropylmethylcellulose to the HP-beta-CD solution. The present results suggest that the use of cyclodextrins might be a simple and useful method to overcome the poor water solubility of THC. (C) 1998 Elsevier Science Inc.