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Exercising complementary roles of polymer-coated magnetic nanoparticles for precise drug delivery and image contrast agents has attracted significant attention in biomedical applications. The objective of this study was to prepare and characterize magnetic nanoparticles embedded in polylactide-co-glycolide matrixes (PLGA-MNPs) as a dual drug delivery and imaging system capable of encapsulating both hydrophilic and hydrophobic drugs. PLGA-MNPs were capable of encapsulating both hydrophobic and hydrophilic drugs in a 2:1 ratio. Biocompatibility, cellular uptake, cytotoxicity, membrane potential, and apoptosis were carried out in two different cancer cell lines (MCF-7 and PANC-1). The molecular basis of induction of apoptosis was validated by Western blotting analysis. For targeted delivery of drugs, targeting ligand such as Herceptin was used, and such a conjugated system demonstrated enhanced cellular uptake and an augmented synergistic effect in an in vitro system when compared with native drugs. Magnetic resonance imaging was carried out both in vitro and in vivo to assess the efficacy of PLGA-MNPs as contrast agents. PLGA-MNPs showed a better contrast effect than commercial contrast agents due to higher T(2) relaxivity with a blood circulation half-life ∼ 47 min in the rat model. Thus, our results demonstrated the dual usable purpose of formulated PLGA-MNPs toward either, in therapeutics by delivering different hydrophobic or hydrophilic drugs individually or in combination and imaging for cancer therapeutics in the near future.

The mean particle size ranged from 230 to 360 nm, as measured by dynamic laser light scattering, and scanning-electron microscopy confirmed the spherical nature and smooth surface of the nanoparticles. Fourier transform infrared spectroscopy analysis of void nanoparticles, drug-loaded nanoparticles and native DXY indicated no interaction between the drug and polymer in the nanoparticle. Differential scanning calorimetry analysis of drug-loaded nanoparticles indicated a molecular level dispersion of DXY in the formulation. The antibacterial activity of native DXY and DXY-loaded nanoparticles were tested using a strain of Escherichia coli (DH5alpha) through growth inhibition and colony-counting method. The results indicated that DXY-loaded nanoparticles are more effective than native DXY due to the sustained release of DXY from nanoparticles in the E. coli strain.