한빛사 논문
Jun Young Parka,1, Sanghyo Parkb,1, Tae Sup Leec, Yong Hwa Hwangc, Jung Young Kimc, Won Jun Kanga,*, Jaehong Keyb,*
a Department of Nuclear Medicine, Severance Hospital, Yonsei University College of Medicine, 50-1 Yonsei-ro, Seodaemun-gu, Seoul 03722, Republic of Korea
b Department of Biomedical Engineering, Yonsei University, Wonju, Gangwon-do, 26493, Republic of Korea
c Division of RI Application, Korea Institute of Radiological and Medical Sciences (KIRAMS), Seoul, 01812, Republic of Korea
1 Authors contributed equally.
*Corresponding author : Won Jun Kang, Jaehong Key
Abstract
Various types of particle-based drug delivery systems have been explored for the treatment of pulmonary diseases; however, bio-distribution and elimination of the particles should be monitored for better understanding of their therapeutic efficacy and safety. This study aimed to characterize the biological properties of micro-sized discoidal polymeric particles (DPPs) as lung-targeted drug delivery carriers. DPPs were prepared using a top-down fabrication approach and characterized by assessing size and zeta potential. They were labeled with zirconium-89 (89Zr), and bio-distribution studies and PET imaging were performed for 7 days after intravenous administration. Their hydrodynamic size was 2.8 ± 6.1 μm and average zeta potential was −39.9 ± 5.39 mV. At doses of 5, 12.5, and 25 mg/kg, they showed no acute toxicity in nude mice. Desferrioxamine (DFO)-functionalized 89Zr-labeled DPPs gave a decay-corrected radiochemical yield of 82.1 ± 0.2%. Furthermore, 89Zr-DPPs, from chelate-free labeling methods, showed a yield of 48.5 ± 0.9%. Bio-distribution studies and PET imaging showed 89Zr-DFO-DPPs to be mainly accumulated in the lungs and degraded within 3 d of injection. However, 89Zr-DFO-DPPs showed significantly low uptake in the bone. Overall, our results suggested micro-sized DPPs as promising drug delivery carriers for the targeted treatment of various pulmonary diseases.
Keywords : Drug delivery system; Discoidal polymeric particle; Pulmonary disease; Zr-89; PET imaging
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