Abstract
In this work, we report K237-peptide functionalized hybrid chitosan/poly(N-isopropylacrylamide) nanoparticles (NPs) loaded with paclitaxel (PTX), and explore these for the active targeting and effective treatment of KDR/Flk-1-overexpressing human breast cancer. We find that the peptide-functionalized NPs have favorable pH and temperature-sensitive characteristics, with more rapid drug release at the slighly acidic pH of the tumor microenvironment, and accelerated release at higher temperatures. MTT assays showed that the K237-conjugated NPs could more effectively inhibit breast cancer cell growth than peptide-free NPs. Confocal microscopy experiments showed that the NPs could precisely target MDA-MB-231 human breast cancer cells, which over-express the KDR/Flk-1 protein. This shows that the enhanced efficacy of the K237-functionalized NPs in preventing cell proliferation is likely to be associated with specific recognition of KDR/Flk-1 on the cells by the K237 peptide. These results indicate that the peptide functionalized NPs have potential applications for targeted delivery and the controlled release of anticancer drugs.
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