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

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 crossover human study, showing significant release in the small intestine; (ii) in vivo particle-counting data in rats, 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. The accompanying file contains supplementary material available at https://doi.org/10.1016/j.jconrel.2022.08.017.

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. [Dataset] Journal of controlled release [online], 350, pages 244-255. Available from: https://www.sciencedirect.com/science/article/pii/S0168365922005211?via%3Dihub#s0180

• Acceptance Date: Aug 10, 2022
• Online Publication Date: Aug 24, 2022
• Publication Date: Oct 31, 2022
• Deposit Date: Aug 26, 2022
• Publicly Available Date: Aug 25, 2023
• Publisher: Elsevier
• 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/1740888
• Related Public URLs: https://rgu-repository.worktribe.com/output/1734907
• Type of Data: DOCX file of supplementary information.
• Collection Date: Aug 10, 2022
• Collection Method: Blood samples were withdrawn after fasting (time 0), then at 15, 30, 45, 60, 120, 180 and 240 minutes after taking the supplement. Serum was separated in a refrigerated centrifuge and stored at −80 °C until batch analysis was done. 25OHD was analysed using tandem mass spectrometry, the current gold standard in clinical practice for measurement of 25OHD, with a coefficient of variation of 5%. Area under the curve (AUC0-4h) was used to determine the bioavailability of 25OH vitamin D2 from the two different ergocalciferol preparations. The mean AUC for 25OHD was calculated using the linear trapezoid method, baseline levels were normalised to 0 (Tables S3 a-b). Since the number of subjects was small, potentially jeopardising the strong assumption of normality a non-parametric statistical test, the Wilcoxon signed rank test, was used to compare the 25OHD from two different supplements using SPSS software version 15. Data were recorded as median (interquartile range).