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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; Kruusmägi, Martin; Walther, Thomas; Booth, Jonathan; Boa, Andrew N.; Archibald, Stephen J.; Thompson, Colin; Atkin, Stephen L.; Mackenzie, Grahame

Authors

Alberto Diego-Taboada

Fraser Courts

Farooq Almutairi

Benjamin P. Burke

Kate Harris

Martin Kruusmägi

Thomas Walther

Jonathan Booth

Colin Thompson

Stephen L. Atkin



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., …Mackenzie, G. (2022). Spore exines increase vitamin D clinical bioavailability by mucoadhesion and bile triggered release. Journal of controlled release : official journal of the Controlled Release Society, 350, 244-255. 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 2022-10
Deposit Date Aug 25, 2022
Publicly Available Date Aug 25, 2023
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; Clinical-bioavailability enhancement; Vitamin D; Mucoadhesion; 99mTc-sporopollenin
Public URL https://hull-repository.worktribe.com/output/4060232

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