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The grafting and release behavior of doxorubincin from Fe(3)O(4)@SiO(2) core-shell structure nanoparticles via an acid cleaving amide bond: the potential for magnetic targeting drug delivery
Authors:Chen F H  Gao Q  Ni J Z
Affiliation:State Key Laboratory of Rare Earth Resources and Application, Changchun Institute of Applied Chemistry, Chinese Academy of Sciences, Changchun 130022, People's Republic of China. Graduate University of the Chinese Academy of Sciences, Beijing 100049, People's Republic of China.
Abstract:Fe(3)O(4)@SiO(2) core-shell structure nanoparticles were first prepared and characterized by TEM, FTIR, XPS and XRD. Subsequently the widely used anticancer agent doxorubincin (DOX) was successfully grafted to the surface of the core-shell nanoparticles via an amide bond with the aid of a spacer arm we synthesized. The spacer arm met two needs: one end can couple to the core-shell nanoparticles' surface while the other end was the active?-COOH group, which can react with the?-NH(2) group of DOX molecules. The synthesized spacer arm and the conjugation of the drug with nanoparticles through amidation were confirmed by FTIR. The DOX-loading efficiency determined by UV-vis spectrometer was 86.5%. Drug release experiments displayed a pH-dependent behavior that DOX was cleaved from the nanoparticles easily under low pH conditions in the presence of protease and that most of the conjugated doxorubincin were released within the first 12?h. The prepared DOX-grafted Fe(3)O(4)@SiO(2) core-shell structure nanoparticles showed a superparamagnetic property with a saturation magnetization value of 49.3?emu?g(-1), indicating a great potential application in the treatment of cancer using magnetic targeting drug-delivery technology.
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