Application of a liquisolid technique to cannabis sativa extract compacts: Effect of liquid vehicles on the dissolution enhancement and stability of cannabinoids

• Published in: International journal of pharmaceutics Vol. 612; p. 121277
• Main Authors: Jaipakdee, Napaphak, Tabboon, Peera, Limpongsa, Ekapol
• Format: Journal Article
• Language: English
• Published: Netherlands Elsevier B.V 25.01.2022
• Subjects: Cannabidiol; Cannabinoids; Cannabinol; Cannabis; Cannabis sativa L; Delta-9-tetrahydrocannabinol; Dissolution enhancement; Excipients; Liquisolid tablets; Plant Extracts; Solubility; Tablets; Cannabinol; Delta-9-tetrahydrocannabinol; Cannabidiol; Cannabis sativa L; Dissolution enhancement; Liquisolid tablets
• ISSN: 0378-5173; 1873-3476
• DOI: 10.1016/j.ijpharm.2021.121277

[Display omitted] •Application of liquisolid technique significantly enhanced cannabinoid dissolution.•Different liquid vehicles affected hardness and disintegration to different extents.•Liquid vehicles demonstrated different effects on cannabinoid dissolutions.•Liquid vehicles had no effect on percent cannabinoid remaining of 90-d-old compacts. This work describes the application of liquisolid technique to enhance cannabinoid dissolution from Cannabis sativa L. (CS) compacts. Effects of five vehicles, namely, volatile (ethanol) and nonvolatile (caprylocaproyl macrogolglycerides, polyethylene glycol 400, oleoyl macrogolglycerides and polysorbate 20) liquids, on tablet properties, dissolution and stability were investigated. The viscid oleoresin CS extract was mixed with vehicles before being transformed into free-flowing powder by the use of microcrystalline cellulose and colloidal silica as carrier and coating materials. Liquid vehicles had a nonsignificant effect on liquid load factor of CS extract. CS liquisolid compacts had acceptable tableting properties in terms of weight variation, friability, hardness, content uniformity and disintegration time. Different vehicles affected the hardness, disintegration, and wettability of CS compacts and thus the dissolution behaviors of cannabinoids to different extents. Dissolutions of cannabinoids from CS compacts were rate-limited by the disintegration process. Liquisolid formulations using nonvolatile liquids with low polarity or high hydrophilic-lipophilic balance yielded more than 90% cannabinoid dissolution. Stability studies revealed nonsignificant changes in tablet characteristics, cannabinoid content and dissolutions of CS compacts when stored at 5 ± 3 °C for 3 months. This work presents a general concept of how to successfully formulate CS extract with cannabinoid dissolution enhancement characteristics.