Doxorubicin-doxorubicin conjugate prodrug as drug self-delivery system for intracellular pH-triggered slow release

被引：17

作者：

Li, Jiagen ^{[1
]}

Li, Xinming ^{[1
]}

Liu, Peng ^{[1
]}

机构：

[1] Lanzhou Univ, Coll Chem & Chem Engn, State Key Lab Appl Organ Chem, Lanzhou 730000, Gansu, Peoples R China

来源：

COLLOIDS AND SURFACES B-BIOINTERFACES | 2020年 / 185卷

关键词：

Drug self-delivery system; Slow drug release; Drug-drug conjugate; Carbamate linker; Acid-triggered; Doxorubicin; MULTIDRUG-RESISTANCE; NANOPARTICLES; MICELLES; DOX;

D O I：

10.1016/j.colsurfb.2019.110608

中图分类号：

Q6 [生物物理学];

学科分类号：

071011 ;

摘要：

Drug content and releasing rate are the main determining factors for the drug delivery systems (DDSs). Here, doxorubicin dimer (D-DOXcar) was synthesized as drug-drug conjugate prodrug with high drug content of 86%, via an acid-triggered hydrolysable carbamate linker. The prodrug nanoparticles (D-DOXcar-NP) with different diameters were prepared as drug self-delivery system (DSDS) for intracellular pH-triggered slow release. They showed size- and concentration-dependent pH-triggered slow DOX release. For the D-DOXcar-sNP with smaller diameter, the cumulative release ratio reached 25.6% at pH 5.0 within 60 h. The MTT results demonstrated that the proposed DSDS showed similar tumor inhibition regardless of carboxylesterases, and an enhanced anti-tumor efficacy on the HepG2 cells in comparison with the free DOX.

引用

页数：7