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Poly (ethylene glycol) prodrug for anthracyclines via N-Mannich base linker: Design, synthesis and biological evaluation
Zhao, Yong-Jiang1,2; Wei, Wei1,2; Su, Zhi-Guo1; Ma, Guang-Hui1; Ma, GH
2009-09-08
Source PublicationINTERNATIONAL JOURNAL OF PHARMACEUTICS
ISSN0378-5173
Volume379Issue:1Pages:90-99
AbstractPoly(ethylene glycol)s (PEGs) are potential drug carriers for improving the therapeutic index of anticancer agents. In this work, a novel methodology for constructing PEG prodrug of anthracycline anticancer drugs was developed based on N-Mannich base of salicylamide and its 2-acyloxymethylated derivative. The resultant conjugates first subjected to in vitro hydrolysis testing, which revealed the release behavior of newly synthesized PEG prodrugs could be adjusted by the status of 2-hydroxy group of salicylamide. These PEG prodrugs also demonstrated superior cytotoxicity in antiproliferative assay. O-blocked doxorubicin prodrug with PEG20k as carrier was selected for further in vivo assessments and presented longer circulating life in pharmacokinetic experiment. This high molecular prodrug was also found to be more efficacious against S-180 xenografted tumor than equivalent amount of doxorubicin. (C) 2009 Elsevier B.V. All rights reserved.
KeywordPegylated Prodrug Anthracycline Anticancer Drug N-mannich Base
SubtypeArticle
WOS HeadingsScience & Technology ; Life Sciences & Biomedicine
DOI10.1016/j.ijpharm.2009.06.013
Indexed BySCI
Language英语
WOS KeywordDRUG-DELIVERY SYSTEMS ; IN-VITRO CYTOTOXICITY ; POLYMERIC PRODRUGS ; ANTITUMOR-ACTIVITY ; DOXORUBICIN ; THERAPEUTICS ; RELEASE ; COPOLYMERS ; CONJUGATE ; LINKAGES
WOS Research AreaPharmacology & Pharmacy
WOS SubjectPharmacology & Pharmacy
WOS IDWOS:000269809600012
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Cited Times:19[WOS]   [WOS Record]     [Related Records in WOS]
Document Type期刊论文
Version出版稿
Identifierhttp://ir.ipe.ac.cn/handle/122111/6584
Collection生化工程国家重点实验室
Corresponding AuthorMa, GH
Affiliation1.Chinese Acad Sci, Natl Key Lab Biochem Engn, Inst Proc Engn, Beijing 100190, Peoples R China
2.Chinese Acad Sci, Grad Univ Chinese, Beijing 100049, Peoples R China
Recommended Citation
GB/T 7714
Zhao, Yong-Jiang,Wei, Wei,Su, Zhi-Guo,et al. Poly (ethylene glycol) prodrug for anthracyclines via N-Mannich base linker: Design, synthesis and biological evaluation[J]. INTERNATIONAL JOURNAL OF PHARMACEUTICS,2009,379(1):90-99.
APA Zhao, Yong-Jiang,Wei, Wei,Su, Zhi-Guo,Ma, Guang-Hui,&Ma, GH.(2009).Poly (ethylene glycol) prodrug for anthracyclines via N-Mannich base linker: Design, synthesis and biological evaluation.INTERNATIONAL JOURNAL OF PHARMACEUTICS,379(1),90-99.
MLA Zhao, Yong-Jiang,et al."Poly (ethylene glycol) prodrug for anthracyclines via N-Mannich base linker: Design, synthesis and biological evaluation".INTERNATIONAL JOURNAL OF PHARMACEUTICS 379.1(2009):90-99.
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