Cyclic RGD-Functionalized pH/ROS Dual-Responsive Nanoparticle for Targeted Breast Cancer Therapy

Breast cancer is the most common malignant tumor in women and a big challenge to clinical treatment due high morbidity mortality. The pH/ROS dual-responsive nanoplatforms may be an effective way significantly improve therapeutic efficacy of breast cancer. Herein, we report docetaxel (DTX)-loaded pH/ROS-responsive NP that could achieve active targeting cells selective complete drug release for delivery. NPs were fabricated using nanocarriers consist ROS-responsive moiety (4-hydroxymethylphenylboronic acid pinacol ester, HPAP), cinnamaldehyde (CA, aldehyde organic compound with anticancer activities) cyclodextrin (α-CD). loaded DTX, modified tumor-penetration peptide (circular RGD, cRGD) named DTX/RGD NPs. cRGD promote penetration into deep tissue specifically target cells. After internalization by through receptor-mediated endocytosis, pH-responsive acetal was cleaved CA lysosomal acidic environment. Meanwhile, ROS induced disassembly DTX. In vitro cellular assays verified effectively internalized 4T1 cells, obviously inducing apoptosis, blocking cell cycle consequently, killing vivo animal experiments demonstrated sites inhibit growth mice. Both investigations antitumor effect compared free Thus, provide promising strategy enhancing delivery therapy.