Enhanced Intramuscular Bioavailability of Cannabidiol Using Nanocrystals: Formulation, In Vitro Appraisal, and Pharmacokinetics

Cannabidiol (CBD) has poor water solubility and is subjected to extensive first-pass metabolism. These absorption obstacles are responsible for low and variable oral bioavailability of CBD. This study endeavored to improve CBD bioavailability by intramuscular (IM) injection of CBD nanocrystals (CBD-...

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Published in:AAPS PharmSciTech 2022-03, Vol.23 (3), p.85-85, Article 85
Main Authors: Fu, Xinzhen, Xu, Shiji, Li, Zhi, Chen, Kun, Fan, Huaying, Wang, Yu, Xie, Zeping, Kou, Lijuan, Zhang, Shumin
Format: Article
Language:English
Subjects:
Animals
Biochemistry
Biological Availability
Biomedical and Life Sciences
Biomedicine
Biotechnology
Cannabidiol
Nanoparticles - chemistry
Particle Size
Pharmacology/Toxicology
Pharmacy
Rats
Research Article
Solubility
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Summary:Cannabidiol (CBD) has poor water solubility and is subjected to extensive first-pass metabolism. These absorption obstacles are responsible for low and variable oral bioavailability of CBD. This study endeavored to improve CBD bioavailability by intramuscular (IM) injection of CBD nanocrystals (CBD-NC). The nanocrystals were prepared by antisolvent precipitation method and were characterized in terms of the particle size, polydispersity index (PDI), zeta potential, morphology, and crystalline status. CBD-NC displayed a particle size of 141.7±1.5 nm, a PDI of 0.18±0.01, and a zeta potential of −25.73 mV. CBD-NC freeze-dried powder using bovine serum albumin (BSA) as cryoprotectant had good redispersibility, and the average particle size was 139.1±1.4 nm after reconstitution. Moreover, these freeze-dried powders were characterized for drug loading and pH and were evaluated for in vitro dissolution and in vivo studies in a rat model. The in vivo results showed that AUC 0–24 h and C max of CBD by IM injection of CBD nanocrystals increased significantly compared with that of oral (P.O) administration of CBD nanocrystals and CBD oil solution. This underlines the nano-sized CBD could be suggested as a practical and simple nanosystem for IM delivery with improved bioavailability. More importantly, these results pave the way for future development of CBD-NC retentive dosage forms. Graphical abstract
ISSN:1530-9932
1530-9932
DOI:10.1208/s12249-022-02239-3