Abstract

A reproducible and efficient interfacial polymer disposition method has been used to formulate magnetite/poly(ε-caprolactone) (core/shell) nanoparticles (average size ≈ 125 nm, production performance ≈ 90%). To demonstrate that the iron oxide nuclei were satisfactorily embedded within the polymeric solid matrix, a complete analysis of these nanocomposites by, e.g., electron microscopy visualizations, energy dispersive X-ray spectroscopy, Fourier-transform infrared spectroscopy, electrophoresis, and contact angle goniometry was conducted. The magnetic responsive behaviour of these nanoparticles was quantitatively characterized by the hysteresis cycle and qualitatively investigated by visualization of the colloid under exposure to a 0.4 T magnet. Gemcitabine entrapment into the polymeric shell reported adequate drug loading values (≈11%), and a biphasic and pH-responsive drug release profile (≈four-fold faster Gemcitabine release at pH 5.0 compared to pH 7.4). Cytotoxicity studies in MCF-7 human breast cancer cells proved that the half maximal inhibitory concentration of Gem-loaded nanocomposites was ≈two-fold less than that of the free drug. Therefore, these core/shell nanoparticles could have great possibilities as a magnetically targeted Gemcitabine delivery system for breast cancer treatment.

Highlights

  • IntroductionGemcitabine (Gem) (molecular weight, MW : 299.66 g/mol; water solubility: 22.3 mg/mL; n-octanol-water partition coefficient (log POW ): 0.14) is an effective drug against numerous malignancies

  • Gemcitabine (Gem) (molecular weight, MW : 299.66 g/mol; water solubility: 22.3 mg/mL; n-octanol-water partition coefficient: 0.14) is an effective drug against numerous malignancies.it was approved for the first-line treatment of pancreatic, bladder, breast, and small-cell lung cancers [1]

  • Poly(ε-caprolactone) and Gemcitabine hydrochloride (C9 H12 ClF2 N3 O4 ) were obtained from Merck KGaA (Gernsheim, Germany)

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Summary

Introduction

Gemcitabine (Gem) (molecular weight, MW : 299.66 g/mol; water solubility: 22.3 mg/mL; n-octanol-water partition coefficient (log POW ): 0.14) is an effective drug against numerous malignancies. It was approved for the first-line treatment of pancreatic, bladder, breast, and small-cell lung cancers [1]. The main limitations of this anticancer drug include: (i) rapid metabolism into an inactive molecule, and (ii) a very short half-life (

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