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.

在这项研究中，槲皮素-壳聚糖偶联物（QT-CS）合成用于口服递送阿霉素（DOX），以通过增加其水溶性，打开紧密连接并绕过P-糖蛋白（P-gp）来提高其口服生物利用度。所制备的QT-CS自组装成胶束，可以以高包封率，小粒径（136.9 nm）和强ζ电势（+ 16.2 mV）包封DOX。QT-CS-DOX胶束在胃肠模拟液（pH 1.2 / pH 7.4）中显示出缓释曲线。QT-CS胶束可促进阿霉素的细胞摄取，比游离阿霉素的细胞摄取高2.2倍。载药QT-CS胶束显着降低了Caco-2单层细胞的跨上皮电阻（TEER）值（约57％），从而导致较高的表观通透性系数（阿霉素的P _app）是游离阿霉素的10.17倍。以上结果表明，QT-CS胶束是口服递送不溶性抗癌药物的有前途的载体。