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BioMed Research International
Volume 2013 (2013), Article ID 926584, 8 pages
Research Article

Deposition of Doxorubicin in Rats following Administration of Three Newly Synthesized Doxorubicin Conjugates

1Department of Pharmaceutics, School of Pharmacy, Fourth Military Medical University, Xi’an, Shaan’xi 710032, China
2Department of Obstetrics & Gynecology, PLA General Hospital, Beijing 100853, China
3Department of Clinic Pharmacology, Wuhan General Hospital of Guangzhou Military Area Command, Wuhan, Hubei 430070, China
4Department of Pharmacy, Tangdu Hospital, Fourth Military Medical University, Xi’an, Shaan’xi 710038, China
5Department of Radiation Medicine, School of Public Health, Fourth Military Medical University, Xi’an, Shaan’xi 710032, China
6Department of Neurosurgery, Xijing Hospital, Fourth Military Medical University, Xi’an, Shaan’xi 710032, China

Received 1 October 2013; Accepted 3 November 2013

Academic Editor: Peng Zhang

Copyright © 2013 Menglei Huan 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.


We previously reported the synthesis of three DOX conjugates that represented different targeting vehicles and showed them to have antitumor activity both in vitro and in vivo. However, the relationships between the pharmacokinetics of these DOX conjugates and their chemical structures were not characterized. In the current study, free DOX derived from each of the conjugates was found at low levels in the rat circulatory system, with conjugated DOX being the major form. The two polyethylene glycol (PEG) conjugates slowly released DOX, and 1/2β for total DOX from DOX-LNA, PEG-ami-DOX, and PEG-hyd-DOX was 5.79, 10.22, and 15.18 h, respectively. All three conjugates also deposited less DOX into normal organs than did an equivalent dose of free DOX, and the value of free DOX released by DOX- LNA, PEG-ami-DOX, and PEG-hyd-DOX was 32.5, 9.5, and 4.7 μg/g, respectively. Among the conjugates, the compound with an acid-labile bond between PEG and DOX exhibited the lowest free DOX deposition in healthy tissues, which should decrease the systemic toxicity of free DOX while allowing for tumor targeting by PEG.