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KMID : 0617320020110010252
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Journal of Pharmacetical Sceiences Ewha Womans University
2002 Volume.11 No. 1 p.252 ~ p.258
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Radioisotope carrying polyethylene oxide-polycaprolactone copolymer micelles for targetable bone imaging
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Park, Yoon Jeong
Lee, Jue Yeon/Chang, Young Soo/Jeong, Jae Min/Chung, Jun Key/Lee, Myung Chul/Park, Kyoung Bae
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Abstract
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Tile aim of this research is to develop polymeric micelle system as a targetable bone imaging carriers without nonspecificphagocytosis which is made of polyethylene oxide (PEO) and polycaprolactone (PCL). Diamino-PEO, which has two amino groupsin its structure, was used to conjugate both PCL and ligand for specific radioisotope. PCL was conjugated to one amino group ofdiamino-PEO by using diaminohexyl cyclocarbodiimide (DCC). coupling agent. Hydroxyphenylpropionic acid (HPP).diethylenetriamine pentaacetic acid (DTPA) and mercaptoacetyl glycine glycidyl glycine (MAC3), as ligands for speciflcradioisotopes, were coupled to the rest of amino group of diamino-PEO by the same method as described. Fomation of ligand-conjugated block copolymers, critical micelle concentration (CMC) of the copolymers, hydrodynamic radii. and morphology of themicelles were investigated. Besides, ^125I-labelling efficiency and biodistribution of the micelles were examined. PEO-PCL blockcopolymer micelles demonstrated CMC of 25 mg/l ,and size of 60nm, which may be adequqte for blood vessel and bone imaging.^125I-labelling efficieney was above 90% and was more stable at human serum for 24h. ^125I-1abelled polymeric nicelles showed higherblood maintenance and bone uptake when compared to stannous colloid, used as a control. A noticeable decrease in liver or spleenuptake could be achieved by the micelles. Therefore, radioisotope carrying PEO-PCL micelle system was suggested as a useful toolfor effective diagnostic bone targeting and imaging.02001 Elsrviel´Scietlce Ltd. All rigllts reserved.
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