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Pharmacokinetics of core-polymerized, boron-conjugated micelles designed for boron neutron capture therapy for cancer

Paper ID Volume ID Publish Year Pages File Format Full-Text
6832 520 2012 10 PDF Available
Title
Pharmacokinetics of core-polymerized, boron-conjugated micelles designed for boron neutron capture therapy for cancer
Abstract

Core-polymerized and boron-conjugated micelles (PM micelles) were prepared by free radical copolymerization of a PEG-b-PLA block copolymer bearing an acetal group and a methacryloyl group (acetal-PEG-b-PLA-MA), with 1-(4-vinylbenzyl)-closo-carborane (VB-carborane), and the utility of these micelles as a tumor-targeted boron delivery system was investigated for boron neutron capture therapy (BNCT). Non-polymerized micelles (NPM micelles) that incorporated VB-carborane physically showed significant leakage of VB-carborane (ca. 50%) after 12 h incubation with 10% fetal bovine serum (FBS) at 37 °C. On the other hand, no leakage from the PM micelles was observed even after 48 h of incubation. To clarify the pharmacokinetics of the micelles, 125I (radioisotope)-labeled PM and NPM micelles were administered to colon-26 tumor-bearing BALB/c mice. The 125I-labeled PM micelles showed prolonged blood circulation (area under the concentration curve (AUC): 943.4) than the 125I-labeled NPM micelles (AUC: 495.1), whereas tumor accumulation was similar for both types of micelles (AUCPM micelle: 249.6, AUCNPM micelle: 201.1). In contrast, the tumor accumulation of boron species in the PM micelles (AUC: 268.6) was 7-fold higher than the NPM micelles (AUC: 37.1), determined by ICP-AES. Thermal neutron irradiation yielded tumor growth suppression in the tumor-bearing mice treated with the PM micelles without reduction in body weight. On the basis of these data, the PM micelles represent a promising approach to the creation of boron carrier for BNCT.

Keywords
Boron neutron capture therapy; Poly(ethylene glycol)-block-poly(lactic acid) copolymer; Polymeric micelles; Drug delivery systems; Biodistribution; Nanoparticle-assisted BNCT
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Pharmacokinetics of core-polymerized, boron-conjugated micelles designed for boron neutron capture therapy for cancer
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Publisher
Database: Elsevier - ScienceDirect
Journal: Biomaterials - Volume 33, Issue 13, May 2012, Pages 3568–3577
Authors
, , , , , , , , ,
Subjects
Physical Sciences and Engineering Chemical Engineering Bioengineering
Get Full-Text Now
Don't Miss Today's Special Offer
Price was $35.95
You save - $31
Price after discount Only $4.95
100% Money Back Guarantee
Full-text PDF Download
Online Support
Any Questions? feel free to contact us