Ternary complex of soluble undenatured type II collagen-hydrophobic phytochemical-chondroitin sulfate facilitates high stability and targeted intestinal release properties to active substance

Rong Xu; Yue Gu; David Julian McClements; Lin Zheng; Mingtao Huang; Mouming Zhao

doi:10.1016/j.ijbiomac.2024.138601

Ternary complex of soluble undenatured type II collagen-hydrophobic phytochemical-chondroitin sulfate facilitates high stability and targeted intestinal release properties to active substance

Int J Biol Macromol. 2024 Dec 9:288:138601. doi: 10.1016/j.ijbiomac.2024.138601. Online ahead of print.

Authors

Rong Xu¹, Yue Gu¹, David Julian McClements², Lin Zheng³, Mingtao Huang⁴, Mouming Zhao⁵

Affiliations

¹ School of Food Science and Engineering, South China University of Technology, Guangzhou 510640, China; Guangdong Food Green Processing and Nutrition Regulation Technologies Research Center, Guangzhou 510650, China.
² Department of Food Science, University of Massachusetts, Amherst, MA, USA.
³ School of Food Science and Engineering, South China University of Technology, Guangzhou 510640, China. Electronic address: [email protected].
⁴ School of Food Science and Engineering, South China University of Technology, Guangzhou 510640, China.
⁵ School of Food Science and Engineering, South China University of Technology, Guangzhou 510640, China; Guangdong Food Green Processing and Nutrition Regulation Technologies Research Center, Guangzhou 510650, China; Food Laboratory of Zhongyuan, Luohe 462300, Henan, China. Electronic address: [email protected].

PMID: 39662570
DOI: 10.1016/j.ijbiomac.2024.138601

Abstract

Researchers have reported that soluble undenatured type II collagen (SC II) and hydrophobic phytochemicals (HPs) can ameliorate osteoarthritis (OA) through several mechanisms. However, the solubility of HPs, the stability of SC II, and the bio-accessibility of both need to be greatly improved before they can be successfully used for this purpose. In this study, two common HPs, curcumin (CUR, a hydrophobic polyphenol) and astaxanthin (AST, a carotenoid), were first loaded into SC II, which was then complexed with chondroitin sulfate (CS) to form ternary complexes: SC II-HP-CS. The results showed that SC II had the highest loading capacity for CUR (19.00 ± 0.76 μg/mg) and AST (21.15 ± 1.67 μg/mg) at pH 2.0. The CUR and AST bound to the SC II through non-covalent interactions (mainly hydrophobic interaction) and they both existed in an amorphous form within the complexes. In addition, the binding affinity and hydrophobic interaction between SC II and CUR was higher than those of AST. The thermal stability of the SC II-CUR-CS (T_d = 118.0 ± 2.1 °C) and SC II-AST-CS (T_d = 118.8 ± 3.5 °C) complexes were significantly higher than that of the SC II-CUR (T_d = 104.27 ± 0.28 °C) and SC II-AST (T_d = 103.8 ± 1.6 °C) complexes. SC II-HP complexes dissolved in gastric fluids, resulting in serious degradation of the SC II, while SC II-HP-CS complexes existed in an insoluble form to protect the triple helix structure of SC II (24-46 % retained). The CUR release (94.2 ± 5.8 %) and the free radical scavenging activity (84.6 ± 5.3 %) of SC II-CUR-CS was relatively high after 6 h of intestinal digestion, while AST in SC II-AST and SC II-AST-CS had low solubility and antioxidant activity. Therefore, the ternary complex of SC II-HP-CS was more advantageous as multifunctional delivery systems for the encapsulation, protection, and controlled release of hydrophobic polyphenols, which may provide guidance for the synergistic use of hydrophobic polyphenols and SC II to improve OA.

Keywords: Chondroitin sulfate; Hydrophobic phytochemicals; Soluble undenatured type II collagen; Stability; Targeted intestinal release; Ternary complexes.