Enteric coating of halloysite nanotube/ o-butyrylated chitosan microspheres for the co-delivery of paeoniflorin and butyric acid to colon

Abstract

This study aims to achieve co-delivery of paeoniflorin (PF) and butyric acid (BA) to the colon through Eudragit S100 (EUS100)-coated halloysite nanotube/o-butyryl chitosan microspheres (EUS100-HNT-BUCHNPs). O-butyrylated chitosan (BUCH) was prepared by the acylation reaction of chitosan (CH) and butyric anhydride with methane sulfonic acid as a catalyst. PF-loaded halloysite nanotube/o-butyrylated chitosan microspheres (HNT-BUCHNPs) were prepared by emulsion crosslinking with glutaraldehyde as the crosslinking agent and then coated with EUS100 using the emulsion solvent evaporation method.

X-ray photoelectron spectroscopy (XPS) and scanning electron microscopy results indicated the presence of EUS100 coating on the surface of HNT-BUCHNPs. In vitro release studies demonstrated that the EUS100 coating effectively prevented the release of PF and BA at pH 1.2, while the halloysite nanotube slowed down PF release at pH 6.8. Sequential release experiments in different pH media showed lower release of PF and BA at pH 1.2 and pH 6.8, and higher release at pH 7.4, reaching approximately 80 % and 85 %, respectively.

Gastrointestinal tract retention studies in mice confirmed that EUS100-HNT-BUCHNPs reduced the release of PF and BA in the upper digestive tract, facilitating delivery to the colon. In vivo and in vitro results indicated efficient transport of PF and BA to the colon, suggesting the potential of EUS100-HNT-BUCHNPs as colon-targeted carriers for PF and BA.

Materials

HNT (Al2Si2O5 (OH)4.nH2O, MW: 294.19 Da) was purchased from Guangzhou Runwo Material Technology (Guangzhou, China). Eudragit S100 was provided by Shanghai Dexiang Medicine Tech. (Shanghai, China). PF (>98 %) was purchased from Shanghai Yuanye Bio-Technology (Shanghai, China). CH (degree of deacetylation ≥95 %, viscosity 50–100 mpa.s) was purchased from Shanghai Yien Chemical Technology (Shanghai, China) was purchased from Shanghai Yien Chemical Technology (Shanghai, China).

Haigang Li, Jiaxuan Liu, Lei Zhang, Xinru Zhu, Jing Jiang, Zhaohui Ge, Yifei Zuo, Xiangzhu Chen, Chun Zhang,
Enteric coating of halloysite nanotube/ o-butyrylated chitosan microspheres for the co-delivery of paeoniflorin and butyric acid to colon, Journal of Drug Delivery Science and Technology, Volume 104, 2025, 106508, ISSN 1773-2247, https://doi.org/10.1016/j.jddst.2024.106508.