Multifunctional quercetin conjugated chitosan nano- micelles with P-gp inhibition and permeation enhancement of anticancer drug

被引：86

作者：

Mu, Yuzhi ^{[1
]}

Fu, Yangmu ^{[2
]}

Li, Jing ^{[1
]}

Yu, Xiaoping ^{[1
]}

Li, Yang ^{[1
]}

Wang, Yanan ^{[1
]}

Wu, Xuanjin ^{[1
]}

Zhang, Kaichao ^{[1
]}

Kong, Ming ^{[1
]}

Feng, Chao ^{[1
]}

Chen, Xiguang ^{[1
]}

机构：

[1] Ocean Univ China, Coll Marine Life Sci, 5 Yushan Rd, Qingdao 266003, Shandong, Peoples R China

[2] Chinese Peoples Liberat Army Gen Hosp, Dept Orthopaed, Hainan Branch, Sanya 572013, Hainan, Peoples R China

来源：

CARBOHYDRATE POLYMERS | 2019年 / 203卷

基金：

中国国家自然科学基金;

关键词：

Quercetin; Chitosan; Nano-micelles; Oral delivery; Enhance absorption; IN-VIVO EVALUATION; ORAL DELIVERY; CELLULAR UPTAKE; SURFACE-CHARGE; INTRACELLULAR DELIVERY; NANOPARTICLES; VITRO; EFFICIENT; INSULIN; MUCOADHESION;

D O I：

10.1016/j.carbpol.2018.09.020

中图分类号：

O69 [应用化学];

学科分类号：

081704 ;

摘要：

In this study, quercetin-chitosan conjugate (QT-CS) was synthesized for oral delivery of doxorubicin (DOX) to improve its oral bioavailability by increasing its water solubility, opening tight junction and bypassing the P-glycoprotein (P-gp). The prepared QT-CS self-assembled into micelles which could encapsulate DOX with high encapsulation rate, small particle size (136.9 nm) and strong zeta potential (+16.2 mV). QT-CS-DOX micelles displayed sustained-release profile in gastrointestinal simulation fluid (pH 1.2/pH 7.4). QT-CS micelles could promote cellular uptake of doxorubicin, which was 2.2 folds higher than that of free doxorubicin. The trans epithelial electrical resistance (TEER) value of Caco-2 monolayer cells was significantly reduced (about 57%) by drug loaded QT-CS micelles, leading to a high apparent permeability coefficient (P-app) of doxorubicin, which was 10.17 folds higher than that of free doxorubicin. Above results indicate that QT-CS micelles are promising vehicles for the oral delivery of insoluble anticancer drugs.

引用

页码：10 / 18

页数：9

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