Enhanced Solubility,Stability, and Transcorneal Permeability of Delta-8-Tetrahydrocannabinol in the Presence of Cyclodextrins |
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| Authors: | Ketan Hippalgaonkar Waseem Gul Mahmoud A ElSohly Michael A Repka Soumyajit Majumdar |
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| Institution: | (1) Department of Pharmaceutics, School of Pharmacy, The University of Mississippi, 111 Faser Hall, Oxford, Mississippi 38677, USA;(2) The Research Institute of Pharmaceutical Sciences, The University of Mississippi, Oxford, Mississippi 38677, USA;(3) ElSohly Laboratories, Incorporated, 5 Industrial Park Drive, Oxford, Mississippi 38655, USA; |
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| Abstract: | The purpose of this study was to investigate the effect of cyclodextrins (CDs) on aqueous solubility, stability, and in vitro corneal permeability of delta-8-tetrahydrocannabinol (Δ8-THC). Phase solubility of Δ8-THC was studied in the presence of 2-hydroxypropyl-β-cyclodextrin (HPβCD), randomly methylated-β-cyclodextrin (RMβCD) and
sulfobutyl ether-β-cyclodextrin sodium salt (SβCD). Stability of Δ8-THC in 5% w/v aqueous CD solutions, as a function of pH, was studied following standard protocols. In vitro corneal permeation of Δ8-THC (with and without CDs) across excised rabbit cornea was also determined. Phase-solubility profile of Δ8-THC in the presence of both HPβCD and RMβCD was of the AP type, whereas, with SβCD an AL type was apparent. Aqueous solubility of Δ8-THC increased to 1.65, 2.4, and 0.64 mg/mL in the presence of 25% w/v HPβCD, RMβCD, and SβCD, respectively. Significant degradation of Δ8-THC was not observed within the study period at the pH values studied, except for at pH 1.2. Transcorneal permeation of Δ8-THC was dramatically improved in the presence of CDs. The results demonstrate that CDs significantly increase aqueous solubility,
stability, and transcorneal permeation of Δ8-THC. Thus, topical ophthalmic formulations containing Δ8-THC and modified beta CDs may show markedly improved ocular bioavailability. |
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