Evaluation of amorphous and lipid-based formulation strategies to increase the in vivo cannabidiol bioavailability in piglets.

Koch, Nathan; Jennotte, Olivier; Bourcy, Quentin; Lechanteur, Anna; DEVILLE, Marine; Charlier, Corinne; CHIAP, Patrice; Cardot, J M; Evrard, Brigitte

doi:10.1016/j.ijpharm.2024.124173

Article (Scientific journals)

Evaluation of amorphous and lipid-based formulation strategies to increase the in vivo cannabidiol bioavailability in piglets.

Koch, Nathan; Jennotte, Olivier; Bourcy, Quentin et al.

2024 • In International Journal of Pharmaceutics, 657, p. 124173

Peer Reviewed verified by ORBi

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https://hdl.handle.net/2268/317443

DOI
10.1016/j.ijpharm.2024.124173

PubMed
38685441

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Keywords :

Amorphous; Bioavailability; CBD; Cannabidiol; Lipid-based; Mesoporous silica; in vivo

Abstract :

[en] Cannabidiol (CBD) suffers from poor oral bioavailability due to poor aqueous solubility and high metabolism, and is generally administered in liquid lipid vehicles. Solid-state formulations of CBD have been developed, but their ability to increase the oral bioavailability has not yet been proven in vivo. Various approaches are investigated to increase this bioavailability. This study aimed to demonstrate the enhancement of the oral bioavailability of oral solid dosage forms of amorphous CBD and lipid-based CBD formulation compared to crystalline CBD. Six piglets received the three formulations, in a cross-over design. CBD and 7 - COOH - CBD, a secondary metabolite used as an indicator of hepatic degradation, were analyzed in plasma. A 10.9-fold and 6.8-fold increase in oral bioavailability was observed for the amorphous and lipid formulations, respectively. However, the lipid-based formulation allowed reducing the inter-variability when administered to fasted animals. An entero-hepatic cycle was confirmed for amorphous formulations. Finally, this study showed that the expected protective effect of lipids against hepatic degradation of the lipid-based formulation did not occur, since the ratio CBD/metabolite was higher than that of the amorphous one.

Disciplines :

Pharmacy, pharmacology & toxicology

Author, co-author :

Koch, Nathan ; Université de Liège - ULiège > Département de pharmacie > Pharmacie galénique

Jennotte, Olivier ; Université de Liège - ULiège > Département de pharmacie > Pharmacie galénique

Bourcy, Quentin ; Université de Liège - ULiège > Département de pharmacie > Pharmacie galénique

Lechanteur, Anna ; Université de Liège - ULiège > Département de pharmacie > Pharmacie galénique

DEVILLE, Marine ; Centre Hospitalier Universitaire de Liège - CHU > > Service de toxicologie clinique, médicolégale, environnementale et en entreprise ; Academic Hospital of Liège, Department of Toxicology, GLP-AEPT Unit, Center for Interdisciplinary Research on Medicines (CIRM), Liège 4000, Belgium

Charlier, Corinne ; Université de Liège - ULiège > Département de pharmacie > Chimie toxicologique ; Academic Hospital of Liège, Department of Toxicology, GLP-AEPT Unit, Center for Interdisciplinary Research on Medicines (CIRM), Liège 4000, Belgium

CHIAP, Patrice ; Centre Hospitalier Universitaire de Liège - CHU > > Service de toxicologie clinique, médicolégale, environnementale et en entreprise ; Academic Hospital of Liège, Department of Toxicology, GLP-AEPT Unit, Center for Interdisciplinary Research on Medicines (CIRM), Liège 4000, Belgium

Cardot, J M; Borvo, Ceyrat 63122, France

Evrard, Brigitte ; Université de Liège - ULiège > Département de pharmacie > Pharmacie galénique

Language :

English

Title :

Evaluation of amorphous and lipid-based formulation strategies to increase the in vivo cannabidiol bioavailability in piglets.

Publication date :

27 April 2024

Journal title :

International Journal of Pharmaceutics

ISSN :

0378-5173

eISSN :

1873-3476

Publisher :

Elsevier BV, Netherlands

Volume :

657

Pages :

124173

Peer reviewed :

Peer Reviewed verified by ORBi

Additional URL :

https://api.elsevier.com/content/article/PII:S0378517324004071?httpAccept=text/xml

Funders :

ERDF - European Regional Development Fund
Fonds Léon Fredericq

Available on ORBi :

since 06 May 2024

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