Co-delivery of doxorubicin and curcumin via cRGD-peptide modified MPEG-PLA self-assembly nanomicelles for lung cancer therapy

Abstract Lung cancer is the most common malignancy in the world, with high mortality rate. Nevertheless, therapies to act effectively against lung cancer remain elusive. So far, chemotherapy is still the frontline treatment of lung cancer. Doxorubicin (DOX) is a broad-spectrum anti-tumor drug. However, DOX often has serious side effects and causes multi-drug resistance, which greatly limits its clinical application. In this work, biodegradable methoxy poly(ethylene glycol)-block-poly(lactic acid) (MPEG-PLA) nanomicelles modified by Cyclo(Arg-Gly-Asp-d-Phe-Lys) (cRGD) polypeptide was used for the co-delivery of curcumin (CUR) and DOX (CUR-DOX/cRGD-M). The particle size of the self-assembled drug-loaded nano-micelle approximately was 27.4 nm and the zeta potential was −2.7 mV. Interestingly, CUR can enhance the uptake of DOX by Lewis lung carcinoma (LL/2) cells. The experimental results in vivo and in vitro showed that CUR-DOX/cRGD-M combination therapy could promote apoptosis of lung cancer cells, and conspicuously inhibit the tumor growth. Our data indicate that CUR-DOX/cRGD-M will be biodegradable and sustainable, which may have potential clinical application value in the treatment of lung cancer.