Article ID Journal Published Year Pages File Type
6993 Biomaterials 2012 13 Pages PDF
Abstract

The acidic pH in tumor tissues could be used for targeting solid tumors. In the present study, we designed a tumor-specific pH-responsive peptide H7K(R2)2, which could respond to the acidic pH in tumor tissues, and prepared H7K(R2)2-modified polymeric micelles containing paclitaxel (PTX-PM-H7K(R2)2) in order to evaluate their potential targeting of tumor cells and tumor endothelial cells and their anti-tumor activity in mice with tumor cells. PTX-PM-H7K(R2)2 was prepared by a thin-film hydration method. The in vitro release of PTX from PTX-PM-H7K(R2)2 was tested. The in vitro targeting characteristics of H7K(R2)2-modified polymeric micelles on HUVEC (human umbilical vein endothelial cells) and MCF-7 (human breast adenocarcinoma cells) were evaluated. The in vivo targeting activity of H7K(R2)2-modified polymeric micelles and the in vivo anti-tumor activity of PTX-PM-H7K(R2)2 were also investigated in MCF-7 tumor-bearing mice. The released PTX from the PTX-PM-H7K(R2)2 was not affected by the pH. The targeting activity of the H7K(R2)2-modified polymeric micelles was demonstrated by in vitro flow cytometry and confocal microscopy as well as in vivo biodistribution. PTX-PM-H7K(R2)2 produced very marked anti-tumor and anti-angiogenic activity in MCF-7 tumor-bearing mice in vivo.

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