Citation: Zeyu Li, Huan Shen, Wenli Cai, Quangang Xu, Wei Xia, Keke Ning, Ergang Liu, Yongzhuo Huang. Colon-targeted pellets encapsulating patchouli oil cocrystal for inflammatory bowel disease treatment[J]. Chinese Chemical Letters, ;2026, 37(5): 111292. doi: 10.1016/j.cclet.2025.111292 shu

Colon-targeted pellets encapsulating patchouli oil cocrystal for inflammatory bowel disease treatment

Zeyu Li ^{a, b} ,
Huan Shen ^b ,
Wenli Cai ^{a, b} ,
Quangang Xu ^{b, d} ,
Wei Xia ^{b, e} ,
Keke Ning ^{b, f} ,
Ergang Liu ^{b, *,} ,
Yongzhuo Huang ^{a, b, c, *,}

a.
Key Laboratory of Chronic Disease Prevention and Control of Traditional Chinese Medicine of Guangdong Higher Education Institutes, School of Chinese Materia Medica, Guangzhou University of Chinese Medicine, KLGHEI (2024KSYS024), Guangzhou 510006, China
b.
Zhongshan Institute for Drug Discovery, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Zhongshan 528400, China
c.
Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China
d.
School of Pharmacy, Guizhou Medical University, Guizhou 561113, China
e.
School of Traditional Chinese Pharmacy, Nanjing University of Chinese Medicine, Nanjing 210023, China
f.
Zunyi Medical University, Zunyi 563006, China

liuergang@zidd.ac.cn

yzhuang@simm.ac.cn

Received Date: 12 January 2025
Revised Date: 28 April 2025
Accepted Date: 8 May 2025
Available Online: 10 May 2025

Figures(4)

Patchouli oil (PAO), a traditional herbal remedy with notable anti-inflammatory properties, has demonstrated significant therapeutic potential in gastrointestinal diseases. However, its instability in acidic environments and low bioavailability hinder PAO's clinical application. In this study, we developed a pharmaceutical solid-state form of PAO using a β-cyclodextrin (βCD)-based inclusion cocrystal technology, thus obtaining PAO-βCD cocrystals. PAO-βCD cocrystals exhibited enhanced dissolution and stability. We further encapsulated them in pH-sensitive Eudragit-coated pellets (PAO-βCD@pellet) to achieve site-specific delivery of PAO to the inflamed colon. In vivo results from the dextran sulfate sodium salt (DSS)-induced colitis mouse model showed that PAO-βCD@pellet significantly improved the colonic release of PAO, as evidenced by fluorescence tracking and quantitative analysis of patchouli alcohol, the main active compound of PAO. Furthermore, PAO-βCD@pellet demonstrated superior therapeutic efficacy, reducing disease activity index, preventing intestinal barrier damage, and modulating the gut microbiome. Histological examination confirmed alleviating intestinal epithelial cell damage caused by oxidative stress and inflammation. These findings suggest that PAO-βCD@pellet offers a promising targeted treatment strategy for inflammatory bowel disease (IBD) with enhanced stability, bioavailability, and therapeutic outcomes.
- Patchouli oil,
- Cyclodextrin,
- Inclusion cocrystal,
- Inflammatory bowel disease,
- Colon-targeted delivery
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