期刊
NANOMEDICINE
卷 8, 期 12, 页码 1927-1942出版社
FUTURE MEDICINE LTD
DOI: 10.2217/nnm.12.201
关键词
-dehydrophenylalanine; dipeptide; drug delivery; folic acid; nanoparticle; self-assembly; targeted delivery
资金
- Unesco-Lo'real for Young Women in Science program
- University Grant Commission (New Delhi, India)
- Indian Council of Medical Research (New Delhi, India)
- Department of Science and Technology (New Delhi, India)
- International Centre for Genetic Engineering and Biotechnology (New Delhi, India)
Aim: Different nanoparticles have been investigated to deliver chemotherapeutic agents, but complex synthesis procedures and biocompatibility issues raise concerns in developing them for safe human usage. The aim of this work is to develop ,-dehydrophenylalanine-containing, self-assembled, amphipathic dipeptide nanoparticles for tumor-targeted drug delivery and therapy. Material & methods: Solution-phase peptide synthesis was used to synthesize dipeptides. Nanoparticles were prepared by molecular self-assembly. A tumor distribution study was carried out using a radiolabeling method. Tumor regression studies were carried out in murine ascitic tumors in BALB/c mice and breast tumor xenografts in in nonobese diabetic/severe combined immunonot signdeficiency mice. Results: Arg-,-dehydrophenylalanine formed self-assembled nanoparticles that could be easily derivatized with folic acid. Folic acid-derivatized nanoparticles showed enhanced cellular uptake and, when loaded with doxorubicin, showed enhanced tumor regression compared with underivatized nanoparticles or native drug, without any adverse side effects, both in vitro and in vivo. Original submitted 20 April 2012; Revised submitted 9 November 2012
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