Synthesis of 99mTc-labeled polyaspartic acid/silica nanoassembly as a potential probe for bone imaging

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Abstract Purpose Due to the efficient bone targeting of mesoporous silica nanoparticles (MSNs) and polyaspartic acid (PASP), 99mTc- labeled polyaspartic acid coated mesoporous silica nanoparticles (PASP-mSiO2-DTPA-99mTc) are proposed as a potential probe for bone imaging. Methods Polyaspartic acid-conjugated silica nanoparticles (PASP-mSiO2) were synthesized using aqueous carbodiimide chemistry and characterized by ATR-FTR, FE-SEM, EDX, TEM, TGA and XRD. Radiolabeling of the produced nanoassembly with 99mTc was carried out via a simple DTPA chelation procedure. Aqueous dispersion of the radiolabeled nanoparticles was intravenously injected into normal mice and the bone targeting efficiency was evaluated. Results The PASP-mSiO2 nanoassembly was efficiently synthesized and radiolabeled with 99mTc with a high radiochemical yield (92 ± 0.5%) and sufficient in vitro stability in PBS and FBS for up to 24 h. In vivo biodistribution studies revealed a significant enhancement of radioactivity bone uptake after intravenous injection of PASP-mSiO2-DTPA-99mTc compared to radiolabeled uncoated MSNs (mSiO2-DTPA-99mTc), (13 ± 0.6% IA/gram and 5.4 ± 0.4, respectively). Conclusion PASP endowed MSNs with enhanced biocompatibility and highly selective bone targeting. Therefore, the proposed PASP-mSiO2-DTPA-99mTc nanoassembly has immense potential in the field of bone- imaging via single photon emitting computed tomography (SPECT). Graphical Abstract

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