Fabrication, characterization, and in vitro evaluation of doxorubicin-coupled chitosan oligosaccharide nanoparticles

In this study, we developed pH-sensitive chito-oligosaccharide nano-drug-loaded particles with good bio-compatibility, biodegradation, and controlled drug delivery. Chitosan oligosaccharides (COS), Doxorubicin (DOX) amino groups, and aromatic aldehydes of benzaldehyde-terminated polyethylene glycol were used to spontaneously form pH-sensitive aniline bonds. We aimed to achieve site targeting under weak acidic tumor conditions, improve the efficacy, and reduce the toxic side effects of the drug. Particle size, drug encapsulation efficiency, loading efficiency, and zeta potential of nanoparticles were optimized by altering the ratios of aldehyde, amino groups, and sodium tripolyphosphate. The drug encapsulation efficiency and loading efficiency of COS-DOX1 were 5.55 +/- 0.13% and 88.81 +/- 2.00%, respectively, and the in vitro drug release process displayed a specific pH responsiveness. Co-culture of COS-DOX with HCT-116 human colon cancer cells showed that the nanoparticles exhibited dose-dependent cytotoxicity. At a low dose, COS-DOX1 can promote DOX uptake of tumor cells and exhibit higher cytotoxicity than DOX alone. (C) 2022 Elsevier B.V. All rights reserved.

Automated summary

In this study, pH-sensitive chito-oligosaccharide nano-drug-loaded particles were developed with good bio-compatibility, biodegradation, and controlled drug delivery. The nanoparticles demonstrated site targeting under weak acidic tumor conditions, improved drug efficacy, and reduced toxic side effects.