Abstract

Active targeting of folic acid and passive targeting of magnetic nanoparticles to bring about co-delivery of hydrophobic chemotherapeutic agents were the focus of this work. Co-precipitation in alkaline environment was employed for synthesizing Fe3O4 nanoparticles and stabilized by oleic acid. Aqueous dispersibility of oleic acid coated nanoparticles was brought about by folic acid modified Pluronic F127 and Pluronic F127 mixture. Folic acid is used as a targeting agent which was joined to Pluronic F127 via diethylene glycol bis(3-aminopropyl) ether spacer. The nanocomposite was used to delivery hydrophobic anticancer drugs, paclitaxel, and curcumin. Successful modification at each step was confirmed by FTIR and NMR. Quantitative analysis of attached folic acid indicated a total of 84.34% amount of conjugation. Nanoparticles characterization revealed the hydrodynamic size of and nanocomposite to be 94.2 nm nanometres. Furthermore, transmission electron micrograph reveals the size of the nanoparticle to be 12.5 nm hence also shows the superparamagnetic activity. Drug encapsulation efficiency of 34.7% and 59.5% was noted for paclitaxel and curcumin, respectively. Cytotoxic property of drug-loaded nanocomposites was increased in case of folic acid functionalized nanoparticles and further increased in the presence of an external magnetic field. Cellular uptake increased in the folic acid conjugated sample. Further many folds in the presence of an external magnetic field.Graphic abstract

Highlights

  • Cancer is one of the world’s highly distressing diseases, with 10 million new reports annually (Hamzehalipour Almaki et al 2017)

  • Folic acid (FA)-modified Pluronic F127 (PF127) was prepared in first by modifying PF127 with homofunctionalized diethylene glycol moiety using CDI reagent followed by decoration of FA using zero length cross linkers (EDC and NHS)

  • The addition of Pluronic F127 and Pluronic F127 FA brought about good dispersity and solubility to the composite

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Summary

Introduction

Cancer is one of the world’s highly distressing diseases, with 10 million new reports annually (Hamzehalipour Almaki et al 2017). A promising and growing technology in cancer therapy, involves delivery of chemotherapeutic molecules directly to the site of cancer ensuring restricted drug distribution, enhancement of efficacy and safety of drug (Chauhan and Jain 2013). One such technology gaining importance is nanotechnologybased targeted drug delivery, which allows encapsulating the chemotherapeutic agents and brings about site-specific distribution with a help cancer-specific or a tumor abundant markers for targeting cancer (Veiseh et al 2010; Lomis et al 2016)

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