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Spore exines increase vitamin D clinical bioavailability by mucoadhesion and bile triggered release.

Diego-Taboada, Alberto; Sathyapalan, Thozhukat; Courts, Fraser; Lorch, Mark; Almutairi, Farooq; Burke, Benjamin P.; Harris, Kate; Kruusm�gi, Martin; Walther, Thomas; Booth, Jonathan; Boa, Andrew N.; Archibald, Stephen J.; Thompson, Colin; Atkin, Stephen L.; Mackenzie, Grahame

Authors

Alberto Diego-Taboada

Thozhukat Sathyapalan

Fraser Courts

Mark Lorch

Farooq Almutairi

Benjamin P. Burke

Kate Harris

Martin Kruusm�gi

Thomas Walther

Jonathan Booth

Andrew N. Boa

Stephen J. Archibald

Colin Thompson

Stephen L. Atkin

Grahame Mackenzie



Abstract

Sporopollenin exine capsules (SpECs) are microcapsules derived from the outer shells (exines) of plant spore and pollen grains. This work reports the first clinical study on healthy volunteers to show enhanced bioavailability of vitamin D encapsulated in SpECs from Lycopodium clavatum L. spore grains vs vitamin D alone, and the first evidence (in vitro, ex vivo and in vivo) of mechanisms to account for the enhancement and release of the active in the small intestine. Evidence for mucoadhesion of the SpECs contributing to the mechanism of the enhancement is based on: (i) release profile over time of vitamin D in a double blind cross-over human study showing significant release in the small intestine; (ii) in vivo particle counting data in rat showing preferred retention of SpECs vs synthetic beads; (iii) ex vivo 99mTc labelling and counting data using rat small intestine sections showing preferred retention of SpECs vs synthetic beads; (iv) in vitro mucoadhesion data. Triggered release by bile in the small intestine was shown in vitro using solid state NMR and HPLC.

Citation

DIEGO-TABOADA, A., SATHYAPALAN, T., COURTS, F., LORCH, M., ALMUTAIRI, F., BURKE, B.P., HARRIS, K., KRUUSMÄGI, M., WALTHER, T., BOOTH, J., BOA, A.N., ARCHIBALD, S.J., THOMPSON, C., ATKIN, S.L. and MACKENZIE, G. 2022. Spore exines increase vitamin D clinical bioavailability by mucoadhesion and bile triggered release. Journal of controlled release [online], 350, pages 244-255. Available from: https://doi.org/10.1016/j.jconrel.2022.08.017

Journal Article Type Article
Acceptance Date Aug 10, 2022
Online Publication Date Aug 24, 2022
Publication Date Oct 31, 2022
Deposit Date Aug 22, 2022
Publicly Available Date Mar 28, 2024
Journal Journal of controlled release
Print ISSN 0168-3659
Electronic ISSN 1873-4995
Publisher Elsevier
Peer Reviewed Peer Reviewed
Volume 350
Pages 244-255
DOI https://doi.org/10.1016/j.jconrel.2022.08.017
Keywords Sporopollenin microcapsules; Spore exines; Mucoadhesion; Bile; Vitamin D; Drug delivery systems
Public URL https://rgu-repository.worktribe.com/output/1734907
Related Public URLs https://rgu-repository.worktribe.com/output/1740888

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