Quantitative In Vitro and In Vivo Evaluation of Intestinal and Blood-Brain Barrier Transport Kinetics of the Plant N-Alkylamide Pellitorine
Joint Authors
Veryser, Lieselotte
Bracke, Nathalie
Wynendaele, Evelien
Joshi, Tanmayee
Tatke, Pratima
Taevernier, Lien
De Spiegeleer, Bart
Source
Issue
Vol. 2016, Issue 2016 (31 Dec. 2016), pp.1-11, 11 p.
Publisher
Hindawi Publishing Corporation
Publication Date
2016-07-04
Country of Publication
Egypt
No. of Pages
11
Main Subjects
Abstract EN
Objective.
To evaluate the gut mucosa and blood-brain barrier (BBB) pharmacokinetic permeability properties of the plant N-alkylamide pellitorine.
Methods.
Pure pellitorine and an Anacyclus pyrethrum extract were used to investigate the permeation of pellitorine through (1) a Caco-2 cell monolayer, (2) the rat gut after oral administration, and (3) the BBB in mice after intravenous and intracerebroventricular administration.
A validated bioanalytical UPLC-MS2 method was used to quantify pellitorine.
Results.
Pellitorine was able to cross the Caco-2 cell monolayer from the apical-to-basolateral and from the basolateral-to-apical side with apparent permeability coefficients between 0.6 · 10 - 5 and 4.8 · 10 - 5 cm/h and between 0.3 · 10 - 5 and 5.8 · 10 - 5 cm/h, respectively.
In rats, a serum elimination rate constant of 0.3 h−1 was obtained.
Intravenous injection of pellitorine in mice resulted in a rapid and high permeation of pellitorine through the BBB with a unidirectional influx rate constant of 153 μL/(g·min).
In particular, 97% of pellitorine reached the brain tissue, while only 3% remained in the brain capillaries.
An efflux transfer constant of 0.05 min−1 was obtained.
Conclusion.
Pellitorine shows a good gut permeation and rapidly permeates the BBB once in the blood, indicating a possible role in the treatment of central nervous system diseases.
American Psychological Association (APA)
Veryser, Lieselotte& Bracke, Nathalie& Wynendaele, Evelien& Joshi, Tanmayee& Tatke, Pratima& Taevernier, Lien…[et al.]. 2016. Quantitative In Vitro and In Vivo Evaluation of Intestinal and Blood-Brain Barrier Transport Kinetics of the Plant N-Alkylamide Pellitorine. BioMed Research International،Vol. 2016, no. 2016, pp.1-11.
https://search.emarefa.net/detail/BIM-1098146
Modern Language Association (MLA)
Veryser, Lieselotte…[et al.]. Quantitative In Vitro and In Vivo Evaluation of Intestinal and Blood-Brain Barrier Transport Kinetics of the Plant N-Alkylamide Pellitorine. BioMed Research International No. 2016 (2016), pp.1-11.
https://search.emarefa.net/detail/BIM-1098146
American Medical Association (AMA)
Veryser, Lieselotte& Bracke, Nathalie& Wynendaele, Evelien& Joshi, Tanmayee& Tatke, Pratima& Taevernier, Lien…[et al.]. Quantitative In Vitro and In Vivo Evaluation of Intestinal and Blood-Brain Barrier Transport Kinetics of the Plant N-Alkylamide Pellitorine. BioMed Research International. 2016. Vol. 2016, no. 2016, pp.1-11.
https://search.emarefa.net/detail/BIM-1098146
Data Type
Journal Articles
Language
English
Notes
Includes bibliographical references
Record ID
BIM-1098146