Integrin-targeting thermally cross-linked superparamagnetic iron oxide nanoparticles for combined cancer imaging and drug delivery.
We report multifunctional nanoparticles that are capable of cancer targeting and simultaneous cancer imaging and therapy. The nanoparticles are composed of cyclic arginine-glycine-aspartic acid (cRGD) peptide ligand bioconjugated thermally cross-linked superparamagnetic iron oxide nanoparticles (TCL-SPION) that enable loading of the anticancer drug doxorubicin (Dox). The cyclic RGD-conjugated TCL-SPION (cRGD_TCL-SPION) had a mean hydrodynamic size of 34 ± 8 nm with approximately 0.39 wt% of cyclic RGD attached to the surface of the nanoparticles. The cRGD_TCL-SPION exhibited preferential binding towards target cancer cells (U87MG, integrin α(v)β(3)+) when analyzed by T(2)-weighted magnetic resonance (MR) imaging. When Dox was loaded onto the polymeric coating layers of cRGD_TCL-SPION via ionic interaction, the resulting Dox-loaded cRGD_TCL-SPION (Dox@cRGD_TCL-SPION) showed much higher cytotoxicity in U87MG cells than Dox@TCL-SPION lacking cRGD (IC(50) value of 0.02 µM versus 0.12 µM). These results suggest that Dox@cRGD_TCL-SPION has potential for use as an integrin-targeted, combined imaging and therapeutic agent.
Yu
Mi Kyung
MK
School of Life Sciences, Gwangju Institute of Science and Technology, Gwangju, Republic of Korea.
Park
Jinho
J
Jeong
Yong Yeon
YY
Moon
Woo Kyung
WK
Jon
Sangyong
S
D000970:Antineoplastic Agents / Q000494:pharmacology; D045744:Cell Line, Tumor; D003432:Cross-Linking Reagents / Q000494:pharmacology*; D003952:Diagnostic Imaging / Q000379:methods*; D004317:Doxorubicin / Q000494:pharmacology; D016503:Drug Delivery Systems / Q000379:methods*; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D057446:Hydrodynamics; D055767:Immobilized Proteins / Q000737:chemistry / Q000494:pharmacology; D020128:Inhibitory Concentration 50; D016023:Integrins / Q000378:metabolism*; D008279:Magnetic Resonance Imaging; D058185:Magnetite Nanoparticles / Q000737:chemistry; D018613:Microscopy, Confocal; D010316:Particle Size; D010456:Peptides, Cyclic / Q000138:chemical synthesis / Q000737:chemistry; D013696:Temperature
D000970:Antineoplastic Agents; D003432:Cross-Linking Reagents; D055767:Immobilized Proteins; D016023:Integrins; D058185:Magnetite Nanoparticles; D010456:Peptides, Cyclic; C507169:cyclic arginine-glycine-aspartic acid peptide; D004317:Doxorubicin