Document Detail

Preparation and biological evaluation of tumor-specific Ara-C liposomal preparations containing RGDV motif.
MedLine Citation:
PMID:  23023730     Owner:  NLM     Status:  Publisher    
Arginine-glycine-aspartate (RGD) has been shown to be essential for the recognition of integrins overexpressed in tumor cells, especially during tumor invasion, angiogenesis, and metasis. In this study, a novel tetrapeptide, RGD-valine (RGDV), was designed and attached to the N position of 1-β-d-arabinofuranosylcytosine (Ara-C) at the valine end, as a homing device for the delivery of Ara-C to tumor cells. Furthermore, fatty acids of various chain lengths (C(n) H(2n+1) COOH, n = 7, 9, 11, 13, and 15) were attached to the arginine end of RGDV to form a series of C(n) H(2n+1) CO-RGDV-Ara-C compounds. The structures of C(n) H(2n+1) CO-RGDV-Ara-C compounds were confirmed using mass spectrometry and nuclear magnetic resonance. The liposomal preparations of the synthesized C(n) H(2n+1) CO-RGDV-Ara-C compounds were obtained using the film dispersion method in the presence of phospholipids. The particle size, zeta potential, and dispersity index of the liposomes formed were found to be approximately 215 nm (diameter), approximately -30 mV, and <0.3, respectively. The antitumor activity of the liposomal preparations containing the respective C(n) H(2n+1) CO-RGDV-Ara-C compounds was evaluated in mice inoculated with sarcoma S(180) . Liposomal Ara-C preparation, liposomal C(11) H(23) CO-V-Ara-C preparation, Ara-C, and C(11) H(23) CO-V-Ara-C sodium carboxymethyl cellulose (CMC-Na) suspensions were used as controls. C(n) H(2n+1) CO-RGDV-Ara-C containing liposomal preparations were shown with an enhanced antitumor activity, likely because of the targeting effect of RGDV. © 2012 Wiley Periodicals, Inc. and the American Pharmacists Association J Pharm Sci.
Fei Wang; Chunying Cui; Zhao Ren; Lili Wang; Hu Liu; Guohui Cui
Publication Detail:
Type:  JOURNAL ARTICLE     Date:  2012-9-28
Journal Detail:
Title:  Journal of pharmaceutical sciences     Volume:  -     ISSN:  1520-6017     ISO Abbreviation:  J Pharm Sci     Publication Date:  2012 Sep 
Date Detail:
Created Date:  2012-10-1     Completed Date:  -     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  2985195R     Medline TA:  J Pharm Sci     Country:  -    
Other Details:
Languages:  ENG     Pagination:  -     Citation Subset:  -    
Copyright Information:
Copyright © 2012 Wiley Periodicals, Inc.
School of Chemical Biology and Pharmaceutical Sciences, Capital Medical University, Beijing 100069, China.
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