Cannabis oil formulated in sublingual mucoadhesive matrices

GARCÍA A; BELTRAMINO, C.; TEJADA, G.; CIANCIO, I.; LEONARDI, D.; BARRERA, M. G.

Congreso; 7ma Reunión Internacional de Ciencias Farmacéuticas - RICIFA; 2023

Cannabis oil is currently utilized for a variety of reasons due to its therapeutic benefits and medicinal properties. The precise composition of medical cannabis oil can vary depending on the cannabis strain used and the extraction method applied. Cannabinoids (CBD) exhibit analgesic properties capable of alleviating various types of pain, including chronic pain. They also demonstrate anti-inflammatory properties that are advantageous in the treatment of conditions such as rheumatoid arthritis and inflammatory bowel disease, in addition to their potential for anxiety reduction. The utilization of medical cannabis is regarded as safe, characterized by a relatively low profile of side effects, including drowsiness, dizziness, dry mouth, headache, and anxiety. Cannabis oil is liposoluble, owing to the lipophilic nature of the cannabinoids and terpenes present in the oil. This solubility governs its incorporation into a mucoadhesive matrix for sublingual administration. While the conventional method of administering cannabis oil is in the form of drops, the application of matrices containing the oil via the sublingual route allows for precise dosing of CBD and the direct entry into the bloodstream without hepatic metabolism. The objective of this study was to formulate cannabis oil into adhesive polymeric matrices based on three formulations: 1) a single cationic polymer: Chitosan (Q), 2) a combination of a cationic and anionic polymer: Q and Gum Arabic (GA), and 3) a combination of a cationic and a neutral polymer: Q and Hydroxypropyl Methylcellulose (HPMC), and to characterize these matrices. Cannabis oil was incorporated using two procedures: 1) solubilized in propylene glycol and emulsified with polysorbate 20, and 2) encapsulated within sodium alginate particles through ionic gelation. The matrices were prepared using the casting method and subsequently subjected to characterization. The matrices exhibited favorable macroscopic features, appearing homogeneous and free of lumps, with a slight greenish color resembling that of cannabis oil. They were smooth, flexible, and possessed an appropriate thickness (less than 1 mm) for adherence to the oral mucosa without causing discomfort. The tensile strength of matrices based solely on Q increased when combined with GA, likely due to the formation of primary (ionic) and secondary (electrostatic, hydrogen bonding, and van der Waals forces) interactions. Through their swelling indices, it was determined that matrices formulated from the Q-GA combination in contact with artificial saliva maintained their integrity and exhibited the lowest swelling, and therefore would be the most suitable for placement on the patient's oral mucosa without causing discomfort. In contrast, Q-HPMC matrices showed a high swelling and lost their structure after 20 minutes. Infrared spectra of matrices loaded with cannabis oil displayed characteristic signals at 2922 cm-1, 1743 cm-1y 1464 cm-1, corresponding to cannabis oil, indicating that the cannabis oil remained unaltered during the drying process (40-60 ºC). In conclusion, the Q-GA matrix was able to vehiculize cannabis oil and presented a homogeneous morphology. Among the three matrices developed, the Q-GA-based matrix showed the lowest swelling index, which would not cause discomfort to a potential patient. These matrices could offer an effective and safe alternative for the treatment of chronic or prolonged pain conditions that require the use of cannabis oil.