Abstract

Nanoparticle-mediated drug targeting is an active area of cancer research and hold enormous potential in improving anticancer efficacy by providing tumor tissue specificity. Herein, tumor targeting capabilities of nanoparticles between passive targeting approach via the enhanced permeability and retention (EPR ) effect and active targeting approach via the biotin receptors were compared to determine targeting efficiency rates. For this reason, Fe 3 O 4 @SiO 2 (FITC)-DOX (for passive targeting) and Fe 3 O 4 @SiO 2 (FITC)-BTN/DOX (for active targeting) multifunctional nanoparticles combining imaging and therapy were used. Fluorescence microscopy and flow cytometry were employed to both visualize and quantify the accumulation of nanoparticles into the tumor cells. The results demonstrated that active targeting strategy considerably enhanced nanoparticle accumulation in the cervical carcinoma HeLa cells with a 2-fold increase in comparison to passive targeting. Targeted nanoparticles exhibited higher cytotoxicity in cancer cells with an approximately 2.5-fold better half maximal inhibitory concentration (IC 50 ) value than untargeted nanoparticles. Moreover, it was found that targeted nanoparticles increased the number of apoptotic cells by nearly 21.1% as compared to untargeted nanoparticles. These observations show that active tumor targeting drug delivery systems could be more promising for enhancing the chemotherapeutic effects of anticancer drugs as compared to passive tumor targeting drug delivery systems.

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