Pharmacokinetics of Cannabidiol in Sprague-Dawley Rats After Oral and Pulmonary Administration

Schwotzer, Daniela; Kulpa, Justyna; Trexler, Kristen R.; Dye, Wendy W.; Jantzi, Jacob; Irshad, Hammad; Ware, Mark A.; Bonn‐Miller, Marcel O.; McDonald, Jacob D.; Lefever, Tim

doi:10.1089/can.2022.0121

Cited by 6 publications

(4 citation statements)

References 36 publications

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“…The concentration of CBD in the brain was highest after oral delivery (pulmonary and subcutaneous delivery led to similar peak brain concentrations of CBD). Also in rats, CBD was more rapidly absorbed following inhalation (13.9 mg/kg) than by ingestion when administered with MCT oil by gavage (10 mg/kg; T max 5 min vs. 2 h, respectively) with a 24-fold higher C max and a 15-fold higher AUC [ 11 ]. The C max and AUC of the metabolites 6-OH-CBD, 7-OH-CBD, and 7-COOH-CBD were also higher in the plasma after inhalation than after oral administration of CBD in male rats.…”

Section: Novel Routes Of Cbd Administrationmentioning

confidence: 99%

“…In rats, CBD and its metabolites (6-OH-CBD and 7-OH-CBD) were detected in the whole brain within 5 (CBD) or 30 (metabolites) min after oral dosing (10 mg/kg CBD in MCT). The T max was around 2 h, and the maximal CBD brain exposure was around 100 ng/mL [ 11 ]. Oral administration of CBD (10 mg/kg in sunflower oil) resulted in a peak brain concentration of around 200 ng/g at 2 h after administration [ 20 ].…”

Section: Tissue Distribution Of Cbdmentioning

confidence: 99%

“…For the same relative CBD dose, females consistently showed higher concentrations in the muscle and liver. Repeated pulmonary dosing of CBD over 14 days (6.7 or 13.9 mg/kg) led to quantifiable levels of CBD in the brain measured 24 h after the last dose, while CBD metabolites were only measurable in the brain tissue following the highest inhaled dose (13.9 mg/kg) [ 11 ].…”

Section: Tissue Distribution Of Cbdmentioning

confidence: 99%

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Strategies to Improve Cannabidiol Bioavailability and Drug Delivery

O’Sullivan,

Jensen,

Kolli

et al. 2024

Pharmaceuticals

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The poor physicochemical properties of cannabidiol (CBD) hamper its clinical development. The aim of this review was to examine the literature to identify novel oral products and delivery strategies for CBD, while assessing their clinical implications and translatability. Evaluation of the published literature revealed that oral CBD strategies are primarily focused on lipid-based and emulsion solutions or encapsulations, which improve the overall pharmacokinetics (PK) of CBD. Some emulsion formulations demonstrate more rapid systemic delivery. Variability in the PK effects of different oral CBD products is apparent across species. Several novel administration routes exist for CBD delivery that may offer promise for specific indications. For example, intranasal administration and inhalation allow quick delivery of CBD to the plasma and the brain, whereas transdermal and transmucosal administration routes deliver CBD systemically more slowly. There are limited but promising data on novel delivery routes such as intramuscular and subcutaneous. Very limited data show that CBD is generally well distributed across tissues and that some CBD products enable increased delivery of CBD to different brain regions. However, evidence is limited regarding whether changes in CBD PK profiles and tissue distribution equate to superior therapeutic efficacy across indications and whether specific CBD products might be suited to particular indications.

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Section: Novel Routes Of Cbd Administrationmentioning

confidence: 99%

Section: Tissue Distribution Of Cbdmentioning

confidence: 99%

Section: Tissue Distribution Of Cbdmentioning

confidence: 99%

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Strategies to Improve Cannabidiol Bioavailability and Drug Delivery

O’Sullivan,

Jensen,

Kolli

et al. 2024

Pharmaceuticals

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“…The effects of cannabis vary depending on the formulation, dose, concentration, and route of administration (Schwotzer et al 2022 ; Hlozek et al 2017 ; Grotenhermen 2003 ; Huestis 2007 ). Inhalation, oral, aerosol, transdermal, subcutaneous, rectal, sublingual, intravenous, intraperitoneal, and ocular are all available routes of administration for cannabis products.…”

Section: Introductionmentioning

confidence: 99%

Propylene glycol and Kolliphor as solvents for systemic delivery of cannabinoids via intraperitoneal and subcutaneous routes in preclinical studies: a comparative technical note

et al. 2023

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Background Substance administration to laboratory animals necessitates careful consideration and planning in order to enhance agent distribution while reducing any harmful effects from the technique. There are numerous methods for administering cannabinoids; however, several parameters must be considered, including delivery frequency, volume of administration, vehicle, and the level of competence required for staff to use these routes properly. There is a scarcity of information about the appropriate delivery method for cannabinoids in animal research, particularly those that need the least amount of animal manipulation during the course of the investigation. This study aims to assess the feasibility and potential side effects of intraperitoneal and subcutaneous injection of CBD and THC using propylene glycol or Kolliphor in animal models. By evaluating the ease of use and histopathological side effects of these solvents, this study intends to help researchers better understand an accessible long-term delivery route of administration in animal experiments while minimizing the potential confounding effects of the delivery method on the animal. Methods Intraperitoneal and subcutaneous methods of systemic cannabis administration were tested in rat models. Subcutaneous delivery via needle injection and continuous osmotic pump release were evaluated using propylene glycol or Kolliphor solvents. In addition, the use of a needle injection and a propylene glycol solvent for intraperitoneal (IP) administration was investigated. Skin histopathological changes were evaluated following a trial of subcutaneous injections of cannabinoids utilizing propylene glycol solvent. Discussion Although IP delivery of cannabinoids with propylene glycol as solvent is a viable method and is preferable to oral treatment in order to reduce gastrointestinal tract degradation, it has substantial feasibility limitations. We conclude that subcutaneous delivery utilizing osmotic pumps with Kolliphor as a solvent provides viable and consistent route of administration for long-term systemic cannabinoid delivery in the preclinical context.

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Induction of apoptosis by cannabidiol and its main metabolites in human Leydig cells

Li,

Cournoyer

et al. 2023

Arch Toxicol

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Pharmacokinetics of Cannabidiol in Sprague-Dawley Rats After Oral and Pulmonary Administration

Cited by 6 publications

References 36 publications

Strategies to Improve Cannabidiol Bioavailability and Drug Delivery

Strategies to Improve Cannabidiol Bioavailability and Drug Delivery

Propylene glycol and Kolliphor as solvents for systemic delivery of cannabinoids via intraperitoneal and subcutaneous routes in preclinical studies: a comparative technical note

Induction of apoptosis by cannabidiol and its main metabolites in human Leydig cells

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