NDLI: Deposition of doxorubicin in rats following administration of three newly synthesized doxorubicin conjugates.

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Deposition of doxorubicin in rats following administration of three newly synthesized doxorubicin conjugates.

Content Provider	Europe PMC
Author	Huan, Menglei Tian, Shuang Cui, Han Zhang, Bangle Su, Dan Wang, Jieping Li, Kangchu Cao, Weidong
Copyright Year	2013
Abstract	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 t 1/2 β 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 Cmax 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.
ISSN	23146133
Journal	Biomed Research International
Volume Number	2013
PubMed Central reference number	PMC3870082
PubMed reference number	24381947
e-ISSN	23146141
DOI	10.1155/2013/926584
Language	English
Publisher	Hindawi
Publisher Date	2013-12-05
Access Restriction	Open
Rights License	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. Copyright © 2013 Menglei Huan et al.
Content Type	Text
Resource Type	Article
Subject	Immunology and Microbiology Medicine Biochemistry, Genetics and Molecular Biology

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