The synthesis, self-assembling, and biocompatibility of a novel O-carboxymethyl chitosan cholate decorated with glycyrrhetinic acid

被引：53

作者：

Du, Hongliang ^{[1
]}

Yang, Xiaoye ^{[1
]}

Pang, Xin ^{[1
]}

Zhai, Guangxi ^{[1
]}

机构：

[1] Shandong Univ, Coll Pharm, Dept Pharmaceut, Jinan 250012, Peoples R China

来源：

CARBOHYDRATE POLYMERS | 2014年 / 111卷

关键词：

O-carboxymethylated chitosan; Cholic acid; Glycyrrhetinic acid; Self-aggregates; DRUG-DELIVERY; STEARIC-ACID; NANOPARTICLES; MICELLES; PH; DERIVATIVES; CHITINS; DESIGN;

D O I：

10.1016/j.carbpol.2014.04.095

中图分类号：

O69 [应用化学];

学科分类号：

070301 [无机化学];

摘要：

O-carboxymethyl chitosan (OCMC) was firstly decorated with cholic acid (CA) to acquire an amphiphilic polymer under alkaline condition. Then glycyrrhetinic acid (GA) was conjugated to the polymer via a succinate linker and finally treated with NaCO3 solution to obtain new conjugates for potential liver targeted delivery. These conjugates formed uniform aggregates with low critical aggregation concentrations (0.028-0.079 mg/mL) in PBS. The average diameter of cholic acid modified carboxymethyl chitosan (CMCA) aggregates (110-257 nm) decreased with the increase of CA substitution degree and became slightly larger after GA modification. Negative zeta potential (-15 mV) of GA decorated CMCA (GA-CMCA) revealed that the formation of negatively charged shells and spherical morphology was observed under transmission electron microscopy. Furthermore, hemolysis test, in vitro cytotoxicity assay and cellular uptake study all demonstrated the safety and feasibility of these conjugates as a promising carrier for liver targeted drug delivery. (C) 2014 Elsevier Ltd. All rights reserved.

引用

页码：753 / 761

页数：9

共 37 条

[1]

Beck Ruy C R, 2012, Recent Pat Drug Deliv Formul, V6, P195

[2]

Cancer nanotechnology: The impact of passive and active targeting in the era of modern cancer biology [J].