BLOCK-COPOLYMER OF POLYETHYLENE-GLYCOL AND POLYLYSINE AS A CARRIER OFORGANIC IODINE - DESIGN OF LONG-CIRCULATING PARTICULATE CONTRAST-MEDIUM FOR X-RAY COMPUTED-TOMOGRAPHY

Citation
Vs. Trubetskoy et al., BLOCK-COPOLYMER OF POLYETHYLENE-GLYCOL AND POLYLYSINE AS A CARRIER OFORGANIC IODINE - DESIGN OF LONG-CIRCULATING PARTICULATE CONTRAST-MEDIUM FOR X-RAY COMPUTED-TOMOGRAPHY, Journal of drug targeting., 4(6), 1997, pp. 381-388
Citations number
32
Categorie Soggetti
Pharmacology & Pharmacy
Journal title
ISSN journal
1061186X
Volume
4
Issue
6
Year of publication
1997
Pages
381 - 388
Database
ISI
SICI code
1061-186X(1997)4:6<381:BOPAPA>2.0.ZU;2-8
Abstract
In order to obtain small, polymer-stabilized particulate carriers for organic iodine to serve as a contrast agent for X-ray computed tomogra phy (CT) an attempt was made to design a carrier based on polymeric mi celles. Here we describe the synthesis of an iodine-containing amphiph ilic block-copolymer which. can micellize in aqueous solutions. The tw o blocks of the copolymer consisted of methoxypoly(ethyleneglycol) and poly[epsilon N-(triiodobenzoyl)-L-lysine]. Upon dispersion in water, the:block copolymer formed particles with average diameter 80 nm and i odine content up to 44.7%. The particles start to dissociate to the in dividual polymeric chains in the concentration range of 0.85-0.5 mu M in water at 23 degrees C. Upon intravenous injection at 250 mg of iodi ne/kg (570 mg of the agent/kg) in rabbits the medium demonstrated exce ptional 24 hr half-life in the blood substantiating corona/core struct ure of the particles with PEG chains protecting the iodine-containing core. The possible use of these particulates as contrast medium for X- ray computed tomography is discussed.