Department of Applied Chemistry, Faculty of Engineering, University of Miyazaki, 1-1 Gakuen Kibanadai Nishi, Miyazaki, 889-2192, Japan.
Colloids Surf B Biointerfaces. 2021 Dec;208:112062. doi: 10.1016/j.colsurfb.2021.112062. Epub 2021 Sep 3.
Casein hydrolysate (Pep) is a dispersant for poorly water-soluble drugs and nutraceutical ingredients. However, two types of complexes may be between Pep and poorly water-soluble molecules: those that are (1) dispersed as hydrocolloids in aqueous media with a particle size of 100-500 nm; and (2) not hydrocolloids, as indicated by permeability of the complex through an ultrafiltration (UF) membrane and the fact that the particle size is ambiguous by dynamic light scattering. This study was conducted to clarify the factors that determine the dissolution state of the complexes between poorly water-soluble ingredients and casein hydrolysate. We classified the dissolution state of the complexes between poorly water-soluble ingredients and Pep by the permeability using a UF membrane. Complexes containing larger and more-hydrophobic molecules are hydrocolloids and do not permeate the UF membrane, whereas complexes containing comparatively smaller and less-hydrophobic molecules do permeate the UF membrane. A complex containing indomethacin, which has borderline solubility properties, does not permeate the UF membrane at pH values in which the indomethacin carboxylic acid group is protonated, but it is permeable at pH values in which its carboxylic acid group is deprotonated. Furthermore, we determined the stoichiometry and association constant for the complex between a major peptide in Pep and poorly water-soluble resveratrol (Res) based on fluorescence quenching. We calculated the stoichiometry of Res and PepY to be 2:3 and the association constant to be 2.4 × 10 M.
水解酪蛋白(Pep)是一种用于分散难溶于水的药物和营养成分的分散剂。然而,Pep 与难溶性分子之间可能存在两种类型的复合物:一种是(1)在水介质中分散为胶体,粒径为 100-500nm;另一种是(2)不是胶体,这可以通过复合物通过超滤(UF)膜的渗透性以及动态光散射表明粒径不明确来证明。本研究旨在阐明决定难溶性成分与水解酪蛋白之间复合物溶解状态的因素。我们通过 UF 膜的渗透性对难溶性成分与 Pep 之间复合物的溶解状态进行了分类。含有较大和疏水性更强的分子的复合物是胶体,不会渗透 UF 膜,而含有相对较小和疏水性较弱的分子的复合物则可以渗透 UF 膜。含有吲哚美辛的复合物,其溶解性质处于边界状态,在吲哚美辛羧酸基团质子化的 pH 值下不会渗透 UF 膜,但在其羧酸基团去质子化的 pH 值下是可渗透的。此外,我们还基于荧光猝灭法确定了 Pep 中主要肽与难溶性白藜芦醇(Res)之间复合物的化学计量和缔合常数。我们计算出 Res 和 PepY 的化学计量比为 2:3,缔合常数为 2.4×10^M。