Enhanced antitumor effect of icariin nanoparticles coated with iRGD functionalized erythrocyte membrane

Lung cancer is the most common cause of incidence and mortality among tumor diseases. Icariin (ICA), a potential Chinese medicine monomer, has been reported to show outstanding antitumor effects. However, the hydrophobic nature and less tumor penetration limit its potential as a topical healing agent. There are few studies report the efficacy of ICA on lung cancer, moreover, there is no biomimetic targeted delivery system in the application of ICA. Herein, we firstly develop a novel ICA bionic targeted nano-preparation, camouflaged by the tumor penetrating peptide iRGD (cRGDKGPDC), functionalized red blood cell membrane (RBCM), has the increased solubility, utilized biocompatibility, and aggravated tumor penetration of ICA. In this study, we constructed the iRGD functionalized RBCM mimetic targeted ICA-loaded nanoparticles (iRINPs) and explored the anti-tumor effect of iRINPs against lung cancer with biochemical and behavioral analysis. The results suggested that iRINPs showed improved biocompatibility and stability, and reduced phagocytic uptakes by macrophages. Besides, the modification of iRGD significantly improved the targeting ability of iRINPs. In vitro and in vivo the treatment effects and safety assays showed that iRINPs attained better therapeutic effects than ICA by inhibiting A549 cell migration, proliferation and invasion, as well as reducing side effects of ICA. Overall, we expected that the new bionic nanocarriers would be a promising nano-platform for ICA in the precise therapy of lung cancer.