Cannabidiol: Pharmaceutical formulations and biomedical applications

Cannabidiol (CBD) is a phytocannabinoid compound that can be utilized in different pharmaceutical industries. However, high lipophilicity and extensive first-pass metabolism limit its further applications. Therefore, the development of delivery approaches to overcome these obstacles has been of great interest. Herein, a comprehensive review of CBD, the receptors it targets, pharmacokinetic studies, and pharmaceutical formulations for effective delivery is presented. A comprehensive search was conducted in the Scopus, Web of Science, PubMed, and Google Scholar databases from 2016 to 2025. Different in vitro, in vivo, and clinical studies were included, whereas dissertations and conference abstracts were excluded.The results showed that CBD can target 5-HT1A, TRPV1-4, and PPAR-γ with minimal CB1/CB2 agonistic effects. This is consistent with the fact that CBD is effective in the treatment of epilepsy, pain, inflammation, neuropsychiatric disorders, and cancer without expressing psychoactive effects. Additionally, it was indicated that oral delivery formulations, such as long-chain triglyceride vehicles, self-nanoemulsifying systems, and polymeric/microencapsulated carriers, can improve CBD solubility and accelerate its absorption. Pulmonary delivery provides rapid absorption and is suitable for rapid symptom control, whereas intranasal formulations are suitable for nose-to-brain delivery. Transdermal systems elicit localized anti-inflammatory and neuroprotective effects, whereas transmucosal systems can bypass first-pass metabolism. CBD shows promising therapeutic potential; however, its effects across organs depend primarily on the route of administration. All formulations can be effective, but long-term safety evaluations are necessary.