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Journal of Drug Delivery
Volume 2011, Article ID 349206, 9 pages
http://dx.doi.org/10.1155/2011/349206
Research Article

The Use of Radioactive Marker as a Tool to Evaluate the Drug Release in Plasma and Particle Biodistribution of Block Copolymer Nanoparticles

Celator Pharmaceuticals Inc., 1779 W 75th Avenue, Vancouver, BC, Canada V6P 6P2

Received 15 December 2010; Revised 1 April 2011; Accepted 8 May 2011

Academic Editor: Gerard G. M. D'Souza

Copyright © 2011 Sharon Johnstone et al. This is an open access article distributed under the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

Abstract

Diblock copolymer nanoparticles encapsulating a paclitaxel prodrug, Propac 7, have been used to demonstrate the usefulness of a nonmetabolizable radioactive marker, cholesteryl hexadecyl ether (CHE), to evaluate nanoparticle formulation variables. Since CHE did not exchange out of the nanoparticles, the rate of clearance of the CHE could be used as an indicator of nanoparticle stability in vivo. We simultaneously monitored prodrug circulation and carrier circulation in the plasma and the retention of CHE relative to the retention of prodrug in the plasma was used to distinguish prodrug release from nanoparticle plasma clearance. Nanoparticles labelled with CHE were also used to evaluate accumulation of nanoparticles in the tumour. This marker has provided relevant data which we have applied to optimise our nanoparticle formulations.