Application of Oil-in-Water Cannabidiol Emulsion for the Treatment of Rheumatoid Arthritis

Jelínek, Petr; Roušarová, Jaroslava; Ryšánek, Pavel; Ježková, Martina; Havlůjová, Tereza; Pozniak, J.; Kozlík, Petr; Křížek, Tomáš; Kučera, Tomáš; Šíma, Martin; Slanař, Ondřej; Šoóš, Miroslav

doi:10.1089/can.2022.0176

Cited by 9 publications

(10 citation statements)

References 27 publications

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“…The cross-over study design was chosen because it decreases the impact of inter-individual variability and reduces the number of animals needed for each experiment ( Kralovicova et al, 2022 ). It was already successfully implemented in numerous studies in the recent years ( Boleslavska et al, 2020 ; Hrinova et al, 2022 ; Jelinek et al, 2022 ; Salamunova et al, 2023 ).…”

Section: Methodsmentioning

confidence: 99%

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Ivacaftor pharmacokinetics and lymphatic transport after enteral administration in rats

Pozniak,

Ryšánek,

Smrčka

et al. 2024

Front. Pharmacol.

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Background: Ivacaftor is a modern drug used in the treatment of cystic fibrosis. It is highly lipophilic and exhibits a strong positive food effect. These characteristics can be potentially connected to a pronounced lymphatic transport after oral administration.Methods: A series of studies was conducted to describe the basic pharmacokinetic parameters of ivacaftor in jugular vein cannulated rats when dosed in two distinct formulations: an aqueous suspension and an oil solution. Additionally, an anesthetized mesenteric lymph duct cannulated rat model was studied to precisely assess the extent of lymphatic transport.Results: Mean ± SD ivacaftor oral bioavailability was 18.4 ± 3.2% and 16.2 ± 7.8%, respectively, when administered as an aqueous suspension and an oil solution. The relative contribution of the lymphatic transport to the overall bioavailability was 5.91 ± 1.61% and 4.35 ± 1.84%, respectively.Conclusion: Lymphatic transport plays only a minor role in the process of ivacaftor intestinal absorption, and other factors are, therefore, responsible for its pronounced positive food effect.

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Section: Methodsmentioning

confidence: 99%

“…Lymphatic transport parameters were defined and calculated as previously described ( Rysanek et al, 2020 ; Rysanek et al, 2021 ; Jelinek et al, 2022 ; Salamunova et al, 2023 ). Briefly, absolute bioavailability via lymph (F AL ) was defined as the percentage of the administered drug dose absorbed into the lymph.…”

Section: Methodsmentioning

confidence: 99%

Ivacaftor pharmacokinetics and lymphatic transport after enteral administration in rats

Pozniak,

Ryšánek,

Smrčka

et al. 2024

Front. Pharmacol.

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“…Depending on the emulsifying technology and formulation, the AUC/dose in rodents ranges between 8.2 and 448. Jelinek and colleagues showed that a lecithin-based microemulsion increased CBD bioavailability, with a 3.2-fold higher C max and a 2.1-fold higher AUC than the sunflower-oil-based formulation [ 15 ]. The CBD concentration in the lymph was 2–3 orders of magnitude higher than the serum concentration for both the lecithin-based formulation and the sunflower-oil-based formulation, emphasising their absorption potential.…”

Section: Strategies To Improve the Oral Bioavailability Of Cbd (Precl...mentioning

confidence: 99%

“…In one study in rats, a CBD emulsion demonstrated higher absolute oral bioavailability than an oil solution, with greater lymphatic absorption of CBD [ 15 ]. The same study also showed that the CBD emulsion was therapeutically effective in a model of rheumatoid arthritis.…”

Section: Does An Improved Cbd Pk Profile Lead To Better Efficacy?mentioning

confidence: 99%

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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“…Immunization provokes production of specific collagen-II antibodies, which attack the joint tissue. The onset of polyarthritis in female Wistar rats generally occurs around 10 to 17 days post injection (Holmdahl et al, 2002;Brand et al, 2007;Jelínek et al, 2022).…”

Section: Comparison Of Cia and Ramentioning

confidence: 99%

Pathogenesis of Collagen-Induced Arthritis: Role of Immune Cells with Associated Cytokines and Antibodies, Comparison with Rheumatoid Arthritis

Šteigerová,

Šíma,

Slanař

2023

Fol. Biol.

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Collagen-induced arthritis is the most common in vivo model of rheumatoid arthritis used for investigation of new potential therapies in preclinical research. Rheumatoid arthritis is a systemic inflammatory and autoimmune disease affecting joints, accompanied by significant extra-articular symptoms. The pathogenesis of rheumatoid arthritis and collagen-induced arthritis involves a so far properly unexplored network of immune cells, cytokines, antibodies and other factors. These agents trigger the autoimmune response leading to polyarthritis with cell infiltration, bone and cartilage degeneration and synovial cell proliferation. Our review covers the knowledge about cytokines present in the rat collagen-induced arthritis model and the factors affecting them. In addition, we provide a comparison with rheumatoid arthritis and a description of their important effects on the development of both diseases. We discuss the crucial roles of various immune cells (subtypes of T and B lymphocytes, dendritic cells, monocytes, macrophages), fibroblast-like synoviocytes, and their related cytokines (TNF-α, IL-1β, IL-2, IL-4, IL-6, IL-8, IL-10, IL-12, IL-17, IL-23, GM-CSF, TGF-β). Finally, we also focus on key antibodies (rheumatoid factor, anti-citrullinated protein antibodies, anti-collagen II antibodies) and tissue-degrading enzymes (matrix metalloproteinases).

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Application of Oil-in-Water Cannabidiol Emulsion for the Treatment of Rheumatoid Arthritis

Cited by 9 publications

References 27 publications

Ivacaftor pharmacokinetics and lymphatic transport after enteral administration in rats

Ivacaftor pharmacokinetics and lymphatic transport after enteral administration in rats

Strategies to Improve Cannabidiol Bioavailability and Drug Delivery

Pathogenesis of Collagen-Induced Arthritis: Role of Immune Cells with Associated Cytokines and Antibodies, Comparison with Rheumatoid Arthritis

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