Abstract
A self-assembled peptides-calcium-Vitamin D3 ternary delivery system (CSPH-Ca-VD3) was prepared to investigate the promotion of cellular calcium transport. The constructed CSPH-Ca-VD3 nanocomplex exhibited a spherical structure with a size of 135.2 ± 10.2 nm. Based on the thermodynamic calculation of fluorescent spectra, hydrophobic interaction was shown as the major driving force for this nanocomplex structure. CSPH-Ca-VD3 nanocomplex possessed excellent stability during simulated gastrointestinal digestion, contributing to the prevention of acid degradation of VD3 and the enhancement of calcium solubility. Furthermore, the calcium transport efficiency in the form of CSPH-Ca-VD3 (4 mg/mL) across a Caco-2 cells monolayer was significantly increased 2.3-fold compared to that of free Ca2+, mainly attributed to the upregulation in the presence of CSPH-Ca-VD3 of TRPV6, calbindin D9k and PMCA1b expression in Caco-2 cells. The present study provided a basis for developing a novel delivery system of peptides-calcium chelate with the dual effects of VD3 protection and calcium uptake promotion.
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