Synthesis and Properties of Macrocyclic Butanoic Acid Conjugates as a Promising Delivery Formulation for the Nutrition of Colon

Butanoic acid plays a significant role in the maintenance of mucosal health and is the preferred energy substrate for the cells in the colon. Here, butanoic acid was selectively conjugated to the secondary hydroxyl group of β-cyclodextrin through ester bond using sodium hydride as the deprotonation...

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Main Authors: Jingui Cheng, Benpeng Li, Peipei Ma, Mengying Liu, Zhizhong Wang
Format: Article
Language:English
Published: Wiley 2013-01-01
Series:The Scientific World Journal
Online Access:http://dx.doi.org/10.1155/2013/914234
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author Jingui Cheng
Benpeng Li
Peipei Ma
Mengying Liu
Zhizhong Wang
author_facet Jingui Cheng
Benpeng Li
Peipei Ma
Mengying Liu
Zhizhong Wang
author_sort Jingui Cheng
collection DOAJ
description Butanoic acid plays a significant role in the maintenance of mucosal health and is the preferred energy substrate for the cells in the colon. Here, butanoic acid was selectively conjugated to the secondary hydroxyl group of β-cyclodextrin through ester bond using sodium hydride as the deprotonation reagent. The preliminary release behaviors of butanoic acid in rat gastrointestinal tract contents were investigated at 37°C within 12 h. In the contents of stomach, the conjugates did seldom release butanoic acid, released butanoic acid only 5.8% in the contents of small intestine, and released butanoic acid significantly up to 38.4% in the contents of colon. These results indicate that the conjugate activation took place site specifically in the rat colonic contents, via the biodegradation by glycosidases and hydrolases in the colon. Therefore, the β-cyclodextrin conjugates of butanoic acid may be of value as an orally administered colon-specific formulation for the nutrition of colon.
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institution Kabale University
issn 1537-744X
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spelling doaj-art-a20264997e834eb5882868211f1b0eb32025-08-20T03:38:35ZengWileyThe Scientific World Journal1537-744X2013-01-01201310.1155/2013/914234914234Synthesis and Properties of Macrocyclic Butanoic Acid Conjugates as a Promising Delivery Formulation for the Nutrition of ColonJingui Cheng0Benpeng Li1Peipei Ma2Mengying Liu3Zhizhong Wang4Department of Chemical Engineering, Shihezi University, Shihezi 832003, ChinaSchool of Pharmacy, Ningxia Medical University, Yinchuan 750004, ChinaSchool of Pharmacy, Ningxia Medical University, Yinchuan 750004, ChinaSchool of Pharmacy, Ningxia Medical University, Yinchuan 750004, ChinaSchool of Pharmacy, Ningxia Medical University, Yinchuan 750004, ChinaButanoic acid plays a significant role in the maintenance of mucosal health and is the preferred energy substrate for the cells in the colon. Here, butanoic acid was selectively conjugated to the secondary hydroxyl group of β-cyclodextrin through ester bond using sodium hydride as the deprotonation reagent. The preliminary release behaviors of butanoic acid in rat gastrointestinal tract contents were investigated at 37°C within 12 h. In the contents of stomach, the conjugates did seldom release butanoic acid, released butanoic acid only 5.8% in the contents of small intestine, and released butanoic acid significantly up to 38.4% in the contents of colon. These results indicate that the conjugate activation took place site specifically in the rat colonic contents, via the biodegradation by glycosidases and hydrolases in the colon. Therefore, the β-cyclodextrin conjugates of butanoic acid may be of value as an orally administered colon-specific formulation for the nutrition of colon.http://dx.doi.org/10.1155/2013/914234
spellingShingle Jingui Cheng
Benpeng Li
Peipei Ma
Mengying Liu
Zhizhong Wang
Synthesis and Properties of Macrocyclic Butanoic Acid Conjugates as a Promising Delivery Formulation for the Nutrition of Colon
The Scientific World Journal
title Synthesis and Properties of Macrocyclic Butanoic Acid Conjugates as a Promising Delivery Formulation for the Nutrition of Colon
title_full Synthesis and Properties of Macrocyclic Butanoic Acid Conjugates as a Promising Delivery Formulation for the Nutrition of Colon
title_fullStr Synthesis and Properties of Macrocyclic Butanoic Acid Conjugates as a Promising Delivery Formulation for the Nutrition of Colon
title_full_unstemmed Synthesis and Properties of Macrocyclic Butanoic Acid Conjugates as a Promising Delivery Formulation for the Nutrition of Colon
title_short Synthesis and Properties of Macrocyclic Butanoic Acid Conjugates as a Promising Delivery Formulation for the Nutrition of Colon
title_sort synthesis and properties of macrocyclic butanoic acid conjugates as a promising delivery formulation for the nutrition of colon
url http://dx.doi.org/10.1155/2013/914234
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