title: A pharmacokinetics study of radiolabeled micelles of a poly(ethylene glycol)-block-poly(caprolactone) copolymer in a colon carcinoma-bearing mouse model.
abstract: A copolymer of poly(ethylene glycol)-b-poly(caprolactone) (PEG-PCL) was modified with a benzyl moiety and labeled with I-131. A micelle system, (131)I-benzyl-micelles, formed from (131)I-benzyl-PEG-PCL and PEG-PCL-PC, was created and used for in vitro characterization and in vivo evaluation. Administration of (131)I-benzyl-micelles to a colon carcinoma-bearing mouse model gives a 4.9-fold higher tumor-to-muscle ratio at 48 h post-injection than treatment with the unimer (131)I-benzyl-PEG-PCL. Scintigraphic imaging, biodistribution results and pharmacokinetical evaluation all demonstrated that (131)I-benzyl-micelles are a plausible radioactive surrogate for PEG-PCL copolymer micelles. Modifying the amphiphilic copolymer with a benzyl moiety and labeled it with iodine-131 should make possible the real-time and noninvasive evaluation of the pharmacokinetics of copolymer micelles in vivo.
authors.affiliation: Department of Biomedical Imaging and Radiological Sciences, National Yang-Ming University, Taipei, Taiwan.
authors.forename: Hao-Wen
authors.initials: HW
authors.lastname: Kao
authors.forename: Chi-Jen
authors.initials: CJ
authors.lastname: Chan
authors.forename: Yuan-Chia
authors.initials: YC
authors.lastname: Chang
authors.forename: Yuan-Hung
authors.initials: YH
authors.lastname: Hsu
authors.forename: Maggie
authors.initials: M
authors.lastname: Lu
authors.forename: Jassy
authors.initials: J
authors.lastname: Shian-Jy Wang
authors.forename: Yi-Yu
authors.initials: YY
authors.lastname: Lin
authors.forename: Shyh-Jen
authors.initials: SJ
authors.lastname: Wang
authors.forename: Hsin-Ell
authors.initials: HE
authors.lastname: Wang
mesh_terms: D000818:Animals; D003110:Colonic Neoplasms / Q000378:metabolism*; D004195:Disease Models, Animal; D008297:Male; D051379:Mice; D008807:Mice, Inbred BALB C; D008823:Micelles; D011091:Polyesters / Q000493:pharmacokinetics*; D011092:Polyethylene Glycols / Q000493:pharmacokinetics*; D011877:Radionuclide Imaging; D014018:Tissue Distribution
chemical_list: D008823:Micelles; D011091:Polyesters; C016240:polycaprolactone; D011092:Polyethylene Glycols
keywords: Nanoscale drug carrier; Pharmacokinetics; Radiolabeled micelle; Scintigraphic imaging