Towards Better Delivery of Cannabidiol (CBD)

Abstract

Cannabidiol (CBD) has substantial therapeutic potential, but its development as an effective drug by the pharmaceutical industry is hindered by intrinsic characteristics such as low bioavailability, low water solubility, and variable pharmacokinetic profiles. Importantly, lack of patentability of the drug substance also limits the likelihood of an expensive, full development programme in anything other than orphan indications. Potential avenues to overcome these issues with CBD include self-emulsifying drug delivery systems, improved crystal formulations and other solid-state delivery formulations, which are mostly in the pre-clinical or early clinical stages of development. This review identifies issues compromising current delivery of solid-state CBD, and how advanced pharmaceutical development strategies can enable CBD to realise the full potential as a successful therapeutic agent.

Comparison of Five Oral Cannabidiol Preparations in Adult Humans: Pharmacokinetics, Body Composition, and Heart Rate Variability

“…The high degree of variability in CBD absorption and the resulting pharmacokinetic parameters following CBD ingestion have been previously described [4,12,[18][19][20]. Potential explanations for variable, and often poor, CBD absorption have pertained to properties of the CBD itself (e.g., poor water solubility) and also variability brought about by the significant first pass metabolism it must endure following oral ingestion.…”

“…Following a screening visit consisting of a review of medical history and assessment of body composition, participants reported to the laboratory on five separate mornings in a crossover design. In light of the considerable variability in CBD absorption and the resulting pharmacokinetic parameters following CBD ingestion [4,12,[18][19][20], a crossover design was employed in an attempt to minimize the influence of inter-individual variability. Each morning began with a baseline blood sample and determination of blood pressure, and heart rate variability.…”

“…Despite the enthusiasm of the CBD industry for these claims, the empirical evidence supporting favorable physiological responses is inconsistent [2,3]. These discrepancies may in part be explained by differences in CBD bioavailability when administered orally [4], that in turn may be influenced by non-standardized CBD formulation, and/or the body size and composition of the recipient. With regards to the former, differences in formulation might include water vs. lipid solubility, administration as a food vs. a beverage, co-administration with additional ingredients, and/or preparation as a ready-made product vs. a powder to be mixed with liquid by the consumer before ingestion.…”

Efficacy of Cannabidiol for Δ-9-Tetrahydrocannabinol-Induced Psychotic Symptoms, Schizophrenia, and Cannabis Use Disorders: A Narrative Review

“…These results could also be useful in defining the target dose and ideal length of CBD treatment for these conditions, given the heterogeneous dosages ranging between 200 and 1000 mg and the different treatment durations tested so far. In addition, considering the high variability in the bioavailability of CBD, depending on the route of administration, future research should clarify which are the best treatment approaches for CBD [ 61 ].…”

Cannabidiol (CBD) repurposing as antibacterial: promising therapy of CBD plus polymyxin B against superbugs

“…The clinical CBD pharmacokinetics studies following oral administration were evaluated in different formulations such as capsules, solutions and oromucosal preparations (42,43).…”