کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
2485648 | 1114362 | 2012 | 10 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Preparation and biological evaluation of tumor-specific Ara-C liposomal preparations containing RGDV motif
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کلمات کلیدی
موضوعات مرتبط
علوم پزشکی و سلامت
داروسازی، سم شناسی و علوم دارویی
اکتشاف دارویی
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
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 (CnH2n+1COOH, n = 7, 9, 11, 13, and 15) were attached to the arginine end of RGDV to form a series of CnH2n+1CO-RGDV-Ara-C compounds. The structures of CnH2n+1CO-RGDV-Ara-C compounds were confirmed using mass spectrometry and nuclear magnetic resonance. The liposomal preparations of the synthesized CnH2n+1CO-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 â30 mV, and <0.3, respectively. The antitumor activity of the liposomal preparations containing the respective CnH2n+1CO-RGDV-Ara-C compounds was evaluated in mice inoculated with sarcoma S180. Liposomal Ara-C preparation, liposomal C11H23CO-V-Ara-C preparation, Ara-C, and C11H23CO-V-Ara-C sodium carboxymethyl cellulose (CMC-Na) suspensions were used as controls. CnH2n+1CO-RGDV-Ara-C containing liposomal preparations were shown with an enhanced antitumor activity, likely because of the targeting effect of RGDV.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Journal of Pharmaceutical Sciences - Volume 101, Issue 12, December 2012, Pages 4559-4568
Journal: Journal of Pharmaceutical Sciences - Volume 101, Issue 12, December 2012, Pages 4559-4568
نویسندگان
Fei Wang, Chunying Cui, Zhao Ren, Lili Wang, H.u. Liu, Guohui Cui,