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壳聚糖-果胶聚电解质复合物作为结肠靶向给药载体

Chitosan-pectin polyelectrolyte complex as a carrier for colon targeted drug delivery.

作者信息

Pandey Sonia, Mishra Ashish, Raval Pooja, Patel Hetal, Gupta Arti, Shah Dinesh

机构信息

Maliba Pharmacy College, Surat, Gujarat 394350, India.

出版信息

J Young Pharm. 2013 Dec;5(4):160-6. doi: 10.1016/j.jyp.2013.11.002. Epub 2013 Dec 28.


DOI:10.1016/j.jyp.2013.11.002
PMID:24563596
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC3930120/
Abstract

OBJECTIVE: The objective of present work was to prepare a polyelectrolyte complex (PEC) between chitosan (polycation) & pectin (polyanion) and to develop enteric coated tablets for colon delivery using the PEC. METHODOLOGY: The PECs were prepared using different concentrations of chitosan and pectin. Drug loaded enteric coated tablets were prepared by wet granulation method using PEC to sustain the release at colon and coating was done with Eudragit S 100 to prevent the early release of the drug in stomach and intestine. Two independent variable, % PEC (chitosan/pectin) and % coating were optimized by 3(2) full factorial design. Statistical model were also used to supplement the optimization. DSC was performed to confirm the interaction between the polyions. Developed formulations were evaluated for physical appearance, weight variation, thickness, hardness, friability, % swelling, assay, in-vitro and ex-vivo drug release studies to investigate the PEC's ability to deliver the drug to colon. Ex-vivo release study using rat caecal content was also carried out on optimized formulation. RESULTS AND DISCUSSION: DSC results confirmed chitosan/pectin interaction and subsequent formation of PEC. The optimized formulation containing 1.1% of PEC and 3% of coating showed highest swelling and release in alkaline pH mechanism of which was found to be microbial enzyme dependent degradation established by ex-vivo study using rat caecal content.

摘要

目的:本研究的目的是制备壳聚糖(聚阳离子)与果胶(聚阴离子)之间的聚电解质复合物(PEC),并使用该PEC开发用于结肠给药的肠溶包衣片。 方法:使用不同浓度的壳聚糖和果胶制备PEC。采用湿法制粒法,以PEC为辅料制备载药肠溶包衣片,以实现药物在结肠的缓释,并使用尤特奇S100进行包衣,以防止药物在胃和肠道中过早释放。通过3(2)全因子设计优化了两个自变量,即PEC的百分比(壳聚糖/果胶)和包衣的百分比。还使用统计模型来辅助优化。进行差示扫描量热法(DSC)以确认聚离子之间的相互作用。对所开发的制剂进行外观、重量差异、厚度、硬度、脆碎度、膨胀率、含量测定、体外和离体药物释放研究,以考察PEC将药物递送至结肠的能力。还对优化后的制剂进行了使用大鼠盲肠内容物的离体释放研究。 结果与讨论:DSC结果证实了壳聚糖/果胶之间的相互作用以及随后PEC的形成。含有1.1%PEC和3%包衣的优化制剂在碱性pH值下显示出最高的膨胀率和释放率,其机制被发现是依赖于微生物酶降解的,这是通过使用大鼠盲肠内容物的离体研究所确定的。

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[5]
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[6]
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[7]
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[8]
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[9]
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[10]
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本文引用的文献

[1]
In vitro controlled release of colon targeted mesalamine from compritol ATO 888 based matrix tablets using factorial design.

Res Pharm Sci. 2009-7

[2]
Chitosan/pectin polyelectrolyte complexes: selection of suitable preparative conditions for colon-specific delivery of vancomycin.

Eur J Pharm Sci. 2008-12-18

[3]
Characterisation and controlled drug release from novel drug-loaded hydrogels.

Eur J Pharm Biopharm. 2008-8

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Perspectives of biodegradable natural polysaccharides for site-specific drug delivery to the colon.

J Pharm Pharm Sci. 2007

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Preparation and characterization of free mixed-film of pectin/chitosan/Eudragit RS intended for sigmoidal drug delivery.

Eur J Pharm Biopharm. 2007-8

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Modeling of drug release from delivery systems based on hydroxypropyl methylcellulose (HPMC).

Adv Drug Deliv Rev. 2001-6-11

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