Document Detail


A novel approach to deliver anticancer drugs to key cell types in tumors using a PDGF receptor-binding cyclic peptide containing carrier.
MedLine Citation:
PMID:  20362019     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
Tumor stromal cells have been recently recognized to contribute to tumor growth. Therefore, we hypothesized that delivery of anticancer drugs to these cells in addition to the tumor cells might treat cancer more effectively. Stromal cells abundantly expressed Platelet-Derived Growth Factor Receptor-beta (PDGFR-beta) in different human tumors as shown with immunohistochemistry. To achieve targeting through PDGFR-beta, we developed a carrier by modifying albumin with a PDGFR-beta recognizing cyclic peptide (pPB-HSA). pPB-HSA specifically bound to PDGFR-beta-expressing 3T3 fibroblasts, C26 and A2780 cancer cells in vitro. Subsequently, doxorubicin was conjugated to pPB-HSA through an acid-sensitive hydrazone linkage. In vitro, Dox-HSA-pPB was taken up by fibroblasts and tumor cells and a short exposure of the conjugate induced cell death in these cells. In vivo, the conjugate rapidly accumulated into PDGFR-beta expressing cells in C26 tumors. Treatment with Dox-HSA-pPB significantly reduced the C26 tumor growth in mice while free doxorubicin treated mice had lower response to the therapy. Furthermore, in contrast to free doxorubicin the conjugate did not induce loss in body weight. In conclusion, the present study reveals a novel approach to target key cell types in tumors through PDGFR-beta, which can be applied to enhance the therapeutic efficacy of anticancer drugs.
Authors:
Jai Prakash; Edwin de Jong; Eduard Post; Annette S H Gouw; Leonie Beljaars; Klaas Poelstra
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Publication Detail:
Type:  Comparative Study; Journal Article; Research Support, Non-U.S. Gov't     Date:  2010-03-31
Journal Detail:
Title:  Journal of controlled release : official journal of the Controlled Release Society     Volume:  145     ISSN:  1873-4995     ISO Abbreviation:  J Control Release     Publication Date:  2010 Jul 
Date Detail:
Created Date:  2010-07-12     Completed Date:  2011-01-13     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  8607908     Medline TA:  J Control Release     Country:  Netherlands    
Other Details:
Languages:  eng     Pagination:  91-101     Citation Subset:  IM    
Copyright Information:
Copyright (c) 2010 Elsevier B.V. All rights reserved.
Affiliation:
Department of Pharmacokinetics, Toxicology and Targeting, Groningen Research Institute for Pharmacy, University of Groningen, The Netherlands. J.Prakash@rug.nl
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MeSH Terms
Descriptor/Qualifier:
Animals
Antibiotics, Antineoplastic / pharmacology*
Cell Line, Tumor
Cell Survival / drug effects
Colonic Neoplasms / drug therapy*,  pathology
Doxorubicin / pharmacology*
Female
Humans
Mice
NIH 3T3 Cells
Ovarian Neoplasms / drug therapy*,  pathology
Peptides, Cyclic / genetics,  metabolism,  pharmacology
Receptor, Platelet-Derived Growth Factor beta / metabolism*,  physiology
Serum Albumin / genetics,  metabolism,  pharmacology
Stromal Cells / drug effects,  metabolism*
Chemical
Reg. No./Substance:
0/Antibiotics, Antineoplastic; 0/Peptides, Cyclic; 0/Serum Albumin; 23214-92-8/Doxorubicin; EC 2.7.10.1/Receptor, Platelet-Derived Growth Factor beta
Comments/Corrections
Comment In:
J Control Release. 2010 Jul 14;145(2):75   [PMID:  20576503 ]

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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