Ursodeoxycholic acid grafted chitosan oligosaccharide self-assembled micelles with enhanced oral absorption and antidiabetic effect of oleanolic acid

Oleanolic acid (OA) is a food-derived bioactive component with antidiabetic activity, but its water solubility and oral bioavailability are notably restricted. In this study, to overcome these limitations, ursodeoxycholic acid-modified chitosan oligosaccharide (UCOS) was synthesized to encapsulate O...

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Bibliographic Details
Published in:Food chemistry 2025-04, Vol.470, p.142708, Article 142708
Main Authors: Yuan, Minghao, Wan, Yan, Wang, Yulu, Li, Sihui, Tang, Jiamei, Liang, Xue, Tan, Xin, Yi, Sirui, Wei, Xiaohang, Li, Xiaohong, Guo, Li, Guo, Yiping
Format: Article
Language:English
Subjects:
Chitosan oligosaccharide
Oleanolic acid
Oral delivery
Polymeric micelles
Type 2 diabetes mellitus
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Summary:Oleanolic acid (OA) is a food-derived bioactive component with antidiabetic activity, but its water solubility and oral bioavailability are notably restricted. In this study, to overcome these limitations, ursodeoxycholic acid-modified chitosan oligosaccharide (UCOS) was synthesized to encapsulate OA in self-assembled nanomicelles (UCOS-OA). The encapsulation efficiency and drug loading of UCOS-OA were 86 % and 11 %, respectively. UCOS-OA exhibited enhanced gastrointestinal stability and prolonged intestinal retention time when compared with free OA, resulting in a 10.6-fold increase in oral bioavailability. The enhanced antidiabetic activity of UCOS-OA was confirmed in the type 2 diabetes mellitus mice model, as it significantly improved glycolipid metabolism disorders and mitigated liver injury. Furthermore, UCOS-OA ameliorated the dysbiosis of gut microbiota and fecal metabolites. In conclusion, UCOS serves as an effective polymeric carrier for encapsulating OA, thereby improving its bioavailability and antidiabetic activity. This work provides valuable insights for the advancement of oral delivery systems for bioactive compounds. [Display omitted] •UCOS was synthesized and used as nanocarrier for the oral delivery of OA.•The oral absorption of OA was elevated due to the encapsulation by UCOS.•UCOS-OA showed better antidiabetic activity than free OA.•UCOS-OA alleviated T2DM-induced disorders of gut microbiota and fecal metabolites.
ISSN:0308-8146
1873-7072
1873-7072
DOI:10.1016/j.foodchem.2024.142708