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

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