In vivo evaluation of novel ketal-based oligosaccharides of hyaluronan micelles as multifunctional CD44 receptor-targeting and tumor pH-responsive carriers

Abstract

In this report, the oligosaccharides of hyaluronan (oHA)-histidine-menthone 1,2-glycerol ketal (MGK) (oHM) carried pH-sensitive MGK as hydrophobic moieties and oHA as the target of the CD44 receptor. The oHM could self-assemble, with a diameter of 65 nm. The cellular uptake, indicated by the fluorescent signals, was higher at 4 h. The ex vivo imaging indicated that micelles have a longer blood circulation, beyond 5 h. The fluorescence intensity of the micelles in the liver and spleen was much higher from 5 to 24 h. The CD44 receptor-targeting, indicated by the fluorescence signals of A549 and MDA-MB-231 group, were higher than those of the HepG2 and the control.

Keywords::

• cellular uptake
• CD44 receptor-targeting
• oligosaccharides of hyaluronan
• oHA-histidine-menthone 1,2-glycerol ketal

Declaration of interest

The authors report no declarations of interest. The authors alone are responsible for the content and writing of the paper.

This study is financially supported by the National Natural Science Foundation of China (no.81302718), Taishan Scholar Project (To Dr. Zimei Wu), Young Core Instructor Visitor Foundation of Shandong Province, China (2014), Young Core Instructor Training Program of Yantai University, China (2014).