Chitosan/o-carboxymethyl chitosan nanoparticles for efficient and safe oral anticancer drug delivery: In vitro and in vivo evaluation

被引：264

作者：

Feng, Chao ^{[1
]}

Wang, Zhiguo ^{[2
]}

Jiang, Changqing ^{[3
]}

Kong, Ming ^{[1
]}

Zhou, Xuan ^{[1
]}

Li, Yang ^{[1
]}

Cheng, Xiaojie ^{[1
]}

Chen, Xiguang ^{[1
]}

机构：

[1] Ocean Univ China, Coll Marine Life Sci, Qingdao 266003, Peoples R China

[2] Qingdao Univ, Coll Med, Affiliated Hosp, Qingdao 266003, Peoples R China

[3] Qingdao Municipal Hosp, Qingdao 266003, Peoples R China

来源：

INTERNATIONAL JOURNAL OF PHARMACEUTICS | 2013年 / 457卷 / 01期

基金：

中国国家自然科学基金;

关键词：

Chitosan; Carboxymethyl chitosan; Doxorubicin hydrochloride; pH-responsive; Oral drug delivery; DOXORUBICIN; ABSORPTION;

D O I：

10.1016/j.ijpharm.2013.07.079

中图分类号：

R9 [药学];

学科分类号：

100702 [药剂学];

摘要：

The present study investigated the ability of a polyelectrolyte complex (CS/CMCS-NPs), composed of chitosan (CS) and o-carboxymeymethy chitosan (CMCS) as a pH responsive carrier for oral delivery of doxorubicin hydrochloride (DOX). The obtained CS/CMCS-NPs were characterized for various parameters including morphology, particle size, zeta potential, entrapment efficiency and stability under the simulated GI tract conditions. The pH responsive stability of the DOX-loaded CS/CMCS nanoparticles (DOX: CS/CMCS-NPs) determined the drug release rate, which was lower in acidic pH than the neutral. Ex vivo intestinal adhesion and permeation indicated DOX: CS/CMCS-NGs were able to enhance absorption of DOX throughout the entire small intestine, especially in jejunum and ileum. Oral administration of DOX: CS/CMCS-NPs was effective to deliver DOX into blood, giving an absolute bioavailability of 42%. The tissue distribution and toxicity of DOX: CS/CMCS-NPs in rats showed low level of DOX in heart and kidney, and obviously decreased cardiac and renal toxicities. These results indicated CS/CMCS-NPs were highly efficient and safe as an oral delivery system for DOX. (C) 2013 Elsevier B. V. All rights reserved.

引用

页码：158 / 167

页数：10

共 24 条

[1]

Selective determination of doxorubicin and doxorubicinol in rat plasma by HPLC with photosensitization reaction followed by chemiluminescence detection [J].