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Background Lung cancer is one of the most frequently diagnosed cancers all over the world and is also one of the leading causes of cancer-related mortality. The main treatment option for small cell lung cancer, conventional chemotherapy, is characterized by a lack of specificity, resulting in severe adverse effects. Therefore, this study aimed at developing a new targeted drug delivery (TDD) system based on Ag–In–Zn–S quantum dots (QDs). For this purpose, the QD nanocrystals were modified with 11-mercaptoundecanoic acid (MUA), L-cysteine, and lipoic acid decorated with folic acid (FA) and used as a novel TDD system for targeting doxorubicin (DOX) to folate receptors (FARs) on adenocarcinomic human alveolar basal epithelial cells (A549). NIH/3T3 cells were used as FAR-negative controls. Comprehensive physicochemical, cytotoxicity, and genotoxicity studies were performed to characterize the developed novel TDDs. Results Fourier transformation infrared spectroscopy, dynamic light scattering, and fluorescence quenching confirmed the successful attachment of FA to the QD nanocrystals and of DOX to the QD–FA nanocarriers. UV–Vis analysis helped in determining the amount of FA and DOX covalently anchored to the surface of the QD nanocrystals. Biological screening revealed that the QD–FA–DOX nanoconjugates had higher cytotoxicity in comparison to the other forms of synthesized QD samples, suggesting the cytotoxic effect of DOX liberated from the QD constructs. Contrary to the QD–MUA–FA–DOX nanoconjugates which occurred to be the most cytotoxic against A549 cells among others, no such effect was observed for NIH/3T3 cells, confirming FARs as molecular targets. In vitro scratch assay also revealed significant inhibition of A549 cell migration after treatment with QD–MUA–FA–DOX. The performed studies evidenced that at IC50 all the nanoconjugates induced significantly more DNA breaks than that observed in nontreated cells. Overall, the QD–MUA–FA–DOX nanoconjugates showed the greatest cytotoxicity and genotoxicity, while significantly inhibiting the migratory potential of A549 cells. Conclusion QD–MUA–FA–DOX nanoconjugates can thus be considered as a potential drug delivery system for the effective treatment of adenocarcinomic human alveolar basal epithelial cells.

The development of carbon-encapsulated iron nanoparticles (CEINS) is of considerable interest in many areas of cancer nanotechnology, ranging from basic tumor biology to early detection and treatment of cancer. To meet these challenges, the present study was undertaken to determine the magnetic and relaxometric performance of CEINS used as a new contrast agent for magnetic resonance imaging (MRI) in preclinical phantom models. CEIN samples were synthesized using a carbon arc discharge route, and the as-synthesized nanoparticles were purified and functionalized with surface acidic groups. The presence of various Fe-bearing metallic phases reflecting the net magnetic properties of CEINS was characterized by powder X-ray diffraction (XRD), thermogravimetry (TGA), and vibrating sample magnetometry. The morphological and surface chemistry features were characterized by electron microscopy (transmission electron microscopy [TEM] and scanning electron microscopy [SEM]), Raman spectroscopy, and Fourier transform-infrared (FT-IR) spectroscopy. The textural properties of CEINS, including porosity, surface total charge density, and zeta potentials, were also measured. The as-synthesized different CEIN samples were finally examined as a potent MRI contrast drug candidate. Magnetic resonance relaxation measurements were performed in bovine gelatin-based phantom models by using a 1.5-T MRI scanner equipped with a standard radiofrequency “birdcage” type head coil. To obtain data, T1- and T2-weighted MR images were acquired using the inversion recovery spin echo (SE) and the SE protocol with multiple time of echo (TE), respectively. Chemical characterization showed similarity in morphology and textural properties between as-synthesized CEINS, purified CEINS, and CEINS functionalized with acidic groups. The as-synthesized CEINS had significantly higher Fe content and higher saturation magnetization. The analysis of the relaxometric properties of CEINS revealed that all the CEIN samples decreased T2 relaxation times on the T2-weighted images. The relaxation rate (1/T2) showed some differences between the as-synthesized, purified, and surface-functionalized CEINS containing surface carboxylic groups. Both the as-synthesized and purified CEINS slightly decreased the T1 relaxation times, which was evident through increase in the relaxation rates (1/T1). This study concludes that CEINS may represent a novel “core-shell”–type negative contrast drug candidate for MRI. It should be emphasized that all the studied CEIN samples have acceptable r2 relaxivities at the field strength of 1.5 T where most of the MRI systems operate in clinical radiology.