Abstract: Pingyangmycin(PYM) doped phosphonate-terminated silica nanoparticles(PYM-PO₄SiNP) were prepared via the synchronous modification of functional group in the water-in-oil microemulsion. The effect of the quantum of 3-trihydroxysilylpropyl methylphosphonate(THPMP) on the PYM-PO₄SiNP was investigated. The results show that the ζ potential of PYM-PO₄SiNP decreased obviously, and the release rate of PYM from the PYM-PO₄SiNP accelerated with increase of added THPMP. However, the quantum of THPMP had no impact on the size of PYM-PO₄SiNP. PYM-PO₄SiNP with a good stability and long acting release was prepared with optimal quantum THPMP, at which the drug can release steadily and slowly. The prepared PYM-PO₄SiNP presented drug loading and entrapment efficiency of 7.2% and 37.81%, respectively. The PYM-PO₄SiNP could make the survival rate of CNE-2 cells fell gradually, and PO₄SiNP itself was nontoxic. The research work expands the applications of core/shell silica nanoparticles in the field of drug carrier.

Key words: Drug sustained release, Drug carrier, Pingyangmycine, Phosphonate-terminated silica nanoparticles