Abstract
In this study, we developed pH-sensitive chito-oligosaccharide nano-drug-loaded particles with good biocompatibility, 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.
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