Abstract

Recently, the siderophores have opened new horizons in nanomedicine. The current study aimed to design a theranostic platform based on superparamagnetic iron oxide nanoparticles-pyoverdine (SPION/PVD) conjugates bound to MUC1 aptamer (MUC1Apt) and loaded with doxorubicin (DOX) as an anti-cancer agent. The SPION/PVD complex was covalently conjugated to MUC1Apt and loaded with DOX to prepare a targeted drug delivery system (SPION/PVD/MUC1Apt/DOX). The investigation of cellular cytotoxicity and uptake of formulations by MTT and flow cytometry in both MUC1 positive (C26) and MUC1 negative (CHO) cell lines revealed that MUC1Apt could improve both cellular uptake and toxicity in the C26 cell line. The evaluation of tumor-targeting activity by in vivo bio-distribution showed that the targeted formulation could enhance tumor inhibitory growth effect and survival rate in C26 tumor-bearing mice. Furthermore, the potential of synthesized SPION/PVD/MUC1Apt/DOX complex as diagnostic agents was investigated by magnetic resonance imaging (MRI) which improved the contrast of tumor site in MRI. Our findings confirm that aptamer-targeted PVD chelated the SPION as a diagnostic agent and loaded with DOX as a chemotherapeutic drug, would be beneficial as a novel theranostic platform.

Highlights

  • The siderophores have opened new horizons in nanomedicine

  • As far as we know, this is the first study to provide a superparamagnetic iron oxide NPs (SPIONs)/PVD conjugate as a magnetic resonance imaging (MRI) diagnostic agent which is targeted with an aptamer and loaded with an anti-cancer drug, providing a theranostic platform

  • Our results indicated that while bare SPION is not stable, but PVD/SPIONs/MUC1Apt/DOX is stable enough to be tested in vivo

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Summary

Introduction

The current study aimed to design a theranostic platform based on superparamagnetic iron oxide nanoparticles-pyoverdine (SPION/PVD) conjugates bound to MUC1 aptamer ­(MUC1Apt) and loaded with doxorubicin (DOX) as an anti-cancer agent. A type of MUC1 that is aberrantly overexpressed on the majority of cancer cell surfaces, such as human colon cancer, is commonly mentioned as tumor-associated MUC1 (TA-MUC1) which differs from its normal type in several ­properties[16,17]. These structural differences, have made TA-MUC1 an attractive target for specific diagnosis and treatment of c­ ancers[18,19]

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