Background beta-cyclodextrin modified g-C3N4 (beta-CD/g-C3N4) nanosheets were successfully synthesized and developed as a novel drug carrier of doxorubicin hydrochloride (DOX center dot HCl). The prepared samples were characterized by Fourier transform infrared spectroscopy (FTIR), X-ray diffraction (XRD) and transmission electron microscopy (TEM). The drug-loading and drug release was measured by a UV-visible spectrophotometer. Moreover, cell viability tests were carried out to evaluate the inhibition ratio of beta-CD/g-C3N4-DOX center dot HCl and bulk g-C3N4-DOX center dot HCl. Results The FTIR result confirmed that beta-CD and g-C3N4 are linked by hydrogen bonds. The XRD and TEM results showed that beta-CD/g-C3N4 has nanosheet structure with size range 150-300 nm. The drug-loading ratio rises sharply in the first 14 h and reaches a maximum of 93%. Moreover, beta-CD/g-C3N4 nanocomplex showed a pH-responsive DOX center dot HCl release with a release ratio of 80% at pH = 5, which is two times higher than that of bulk g-C3N4. Cell viability tests demonstrated that the beta-CD/g-C3N4-DOX center dot HCl exhibit a higher inhibition ratio on MG63 cells than bulk g-C3N4-DOX center dot HCl. Conclusion beta-CD/g-C3N4 nanocomplex achieves an ultrahigh drug-loading capacity and pH-responsive release and visualization of the cell phagocytic process. The results indicate that the beta-CD/g-C3N4 nanocomplex can be developed as a promising luminescence carrier for drug delivery. (c) 2018 Society of Chemical Industry