Deposition of Doxorubicin in Rats following Administration of Three Newly Synthesized Doxorubicin Conjugates
Joint Authors
Huan, Menglei
Tian, Shuang
Cui, Han
Zhang, Bangle
Su, Dan
Wang, Jieping
Li, Kangchu
Cao, Weidong
Source
Issue
Vol. 2013, Issue 2013 (31 Dec. 2013), pp.1-8, 8 p.
Publisher
Hindawi Publishing Corporation
Publication Date
2013-12-05
Country of Publication
Egypt
No. of Pages
8
Main Subjects
Abstract EN
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 t1/2β 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 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.
American Psychological Association (APA)
Huan, Menglei& Tian, Shuang& Cui, Han& Zhang, Bangle& Su, Dan& Wang, Jieping…[et al.]. 2013. Deposition of Doxorubicin in Rats following Administration of Three Newly Synthesized Doxorubicin Conjugates. BioMed Research International،Vol. 2013, no. 2013, pp.1-8.
https://search.emarefa.net/detail/BIM-1005435
Modern Language Association (MLA)
Huan, Menglei…[et al.]. Deposition of Doxorubicin in Rats following Administration of Three Newly Synthesized Doxorubicin Conjugates. BioMed Research International No. 2013 (2013), pp.1-8.
https://search.emarefa.net/detail/BIM-1005435
American Medical Association (AMA)
Huan, Menglei& Tian, Shuang& Cui, Han& Zhang, Bangle& Su, Dan& Wang, Jieping…[et al.]. Deposition of Doxorubicin in Rats following Administration of Three Newly Synthesized Doxorubicin Conjugates. BioMed Research International. 2013. Vol. 2013, no. 2013, pp.1-8.
https://search.emarefa.net/detail/BIM-1005435
Data Type
Journal Articles
Language
English
Notes
Includes bibliographical references
Record ID
BIM-1005435