Abstract

The traditional anti-tumor drugs are easily cleared during in vivo circulation and lack of targeting in chemotherapy, thus increasing their side effects and reducing their efficacy. Therefore, a novel acid-labile drug delivery system based on bridged β-cyclodextrins (β-CDs) nano-hydrogel was proposed. β-CD possesses good biocompatibility and hydrophilicity and can be chemically modified to construct a novel bridged complex via pH- responsive carbonic ester bond. In this study, doxorubicin (Dox) was used as an anti-tumor model drug and introduced into this acid-labile bridged β-CD-based nano-hydrogel via non-covalent interactions. The physicochemical properties of acid-labile bridged β-CD-based nano-hydrogel was characterized by 1 Hnuclear magnetic resonance spectra ( 1 HNMR), fourier transform infrared spectra (FTIR), transmission electron microscopy (TEM) and fluorescence spectroscopy. The cell viability and apoptosis of Dox loaded acid-labile bridged β-CD-based nano-hydrogel was obtained by cell counting kit-8 (CCK-8), fluorescence imaging and flow cytometry. The Dox loaded acid-labile bridged β-CD-based nano-hydrogel was stable in normal physiological environment and faster release at pH = 4.5 than that at pH = 7.4 and 9.1. The killing effect on cancerous cells was significantly enhanced in acidic medium compared with that in normal medium. This novel acid-labile bridged β-CD-based nano-hydrogel possesses biosafety and effective anti-cancer strategy, providing significant promising in future biomedical application.