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

• Published in: Journal of controlled release 2022-10, Vol.350, p.244-255
• Main Authors: 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
• Format: Article
• Language: English
• Subjects: 99mTc-sporopollenin; Clinical-bioavailability enhancement; Mucoadhesion; Sporopollenin microcapsules; Vitamin D
• ISSN: 0168-3659; 1873-4995
• DOI: 10.1016/j.jconrel.2022.08.017

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 vivo99mTc 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. [Display omitted] •Clinical-bioavailability enhancement (10 x) of vitamin D in humans by oral route.•Enhanced bioavailability due to mucoadhesion of sporopollenin exine microcapsules.•Release of vitamin D from sporopollenin exine microcapsules triggered by bile.