NOVEL METHODS OF ALTERING PHARMACOKINETICS IN RADIOPHARMACEUTICAL DESIGN
Guest Editor: Hnatowich D. 

The Quarterly Journal of Nuclear Medicine 2002 September;46(3):171-80

Copyright © 2009 EDIZIONI MINERVA MEDICA

lingua: Inglese

Polyethylene glycol in the design of tumor-targetting radiolabelled macromolecules - lessons from liposomes and monoclonal antibodies

Harrington K. J. ¹, Mubashar M. ², Peters A. M. ²

¹ Cancer Research UK Laboratory of Targetted Therapy Centre for Cell and Molecular Biology Institute of Cancer Research, London, UK 2 Department of Nuclear Medicine, Addenbrooke’s Hospital Cambridge, UK

Radiolabelled mac­ro­mol­e­cules ­such as lipo­somes and mono­clo­nal anti­bod­ies (Mab) are attrac­tive ­agents for ­tumour-tar­get­ting stud­ies. In addi­tion to ­their poten­tial diag­nos­tic ­role, ­they can ­also pro­vide ­vital infor­ma­tion on the tar­get­ting capac­ity of ther­a­peu­tic ­agents. Certainly in the ­case of lipo­some devel­op­ment, ­this abil­ity to ­track the phar­ma­cok­i­net­ics and bio­dis­trib­u­tion of the ­agents in a non-inva­sive fash­ion has assist­ed the ­design and appli­ca­tion of ther­a­peu­tic lip­o­so­mal ­agents. A sig­nif­i­cant lim­i­ta­tion of unmod­i­fied lipo­somes and Mab is ­their ten­den­cy to be ­cleared rap­id­ly ­from the cir­cu­la­tion. The use of poly­eth­y­lene gly­col (PEG) in the for­mu­la­tion of ­these ­agents has the capac­ity to ­alter ­their bio­log­i­cal beha­vi­our in ­such a way as to ­improve ­their abil­ity to tar­get ­tumours. In ­this ­paper we ­review the ­data relat­ing to the use of PEG-mod­i­fied lipo­somes and Mab in the con­text of nucle­ar med­i­cine stud­ies.