Contrast agents have been widely used in medicine to enhance contrast in magnetic resonance imaging (MRI). Among them, super paramagnetic iron oxide nanoparticles (SPION) have been reported to have low risk in clinical use. In our study, F127-Folate coated SPION was fabricated in order to efficiently target tumors and provide imaging contrast in MRI. SPION alone have an average core size of 15 nm. After stabilizing with Pluronic F127, the nanoparticles reached a hydrodynamic size of 180 nm and dispersed well in various kinds of media. The F127-Folate coated SPION were shown to specifically target folate receptor expressing cancer cells by flow cytometry analysis, confocal laser scanning microscope, as well as in vitro MRI. Furthermore, in vivo MRI images have shown the enhanced negative contrast from the F127-Folate coated SPION in tumor-bearing mice. In conclusion, our F127-Folate coated SPION have shown great potential as a contrast agent in MRI, as well as in the combination with drug delivery for cancer therapy.

Polymer coating has drawn increasing attention as a leading strategy to overcome the drawbacks of superparamagnetic iron oxide nanoparticles (SPIONs) in targeted delivery of anticancer drugs. In this study, SPIONs were modified with heparin-Poloxamer (HP) shell to form a SPION@HP core-shell system for anticancer drug delivery. The obtained formulation was characterized by techniques including transmission electron microscopy (TEM), Fourier transform infrared spectra (FT-IR), vibration sample magnetometer (VSM), proton nuclear magnetic resonance (¹H-NMR), and powder X-ray diffraction (XRD). Results showed the successful attachment of HP shell on the surface of SPION core and the inability to cause considerable effects to the crystal structure and unique magnetic nature of SPION. The core-shell system maintains the morphological features of SPIONs and the desired size range. Notably, Doxorubicin (DOX), an anticancer drug, was effectively entrapped into the polymeric shell of SPION@HP, showing a loading efficiency of 66.9 ± 2.7% and controlled release up to 120 h without any initial burst effect. Additionally, MTT assay revealed that DOX-loaded SPION@HP exerted great anticancer effect against HeLa cells and could be safely used. These results pave the way for the application of SPION@HP as an effective targeted delivery system for cancer treatment.

The mangosteen peels contain biologically active compounds, with antioxidant and anticancer properties. Among these isolated phytochemicals, α-mangostin is one of the most powerful natural antioxidants and anticancer compounds. This study focused on synthesizing novel α-mangostin (α-MG) derivatives at positions of C-3 and C-6 from extracted α-MG of mangosteen peels and investigating antioxidant and anticancer activities. The structures of the synthesized compounds were determined by using MS, ¹H-NMR, ¹³C-NMR, and HPLC. The analysis of the interaction between structure and bioactivity showed that phenol groups on C-3 and C-6 positions play a crucial role in antiproliferative activity to boost both anticancer efficacy and drug-like properties. The antioxidant activity of α-MG and its derivatives were investigated by the DPPH method. Among α-MG derivatives, 1-hydroxy-7-methoxy-2,8-bis(3-methylbut-2-en-1-yl)-9-oxo-9H-xanthene-3,6-diyl bis(2-bromobenzoate) (compound 4) exhibited significant antioxidant property. The in vitro cytotoxicity against various cancer cell lines (HeLa, MCF-7, NCIH460, and HepG2) was evaluated by the standard sulforhodamine B assay. The anticancer activities (HeLa, MCF-7, NCIH460, and HepG2) of compound 4 are five to six times higher than those of α-MG and other derivatives. The acetylation at C-3 and C-6 of α-MG by halogen of benzoyl greatly improved cancer cell toxicity. Our results provide new opportunities for further explorations of α-MG derivatives for antioxidant property and promise as drugs in cancer therapy.

In this study, a self-assembled nanogel-based pluronic P123-grafted chitosan-folate (CP-FA) was fabricated as a paclitaxel/curcumin codelivery system. ¹H-NMR and TGA proved that the fabricating method of CP-FA was successful. Dynamic light scattering (DLS), zeta potentials, and transmission electron microscopy (TEM) exposed that CP-FA nanoparticles had a uniform size with a diameter of around 16.27±2.01 nm in the colloidal solution and had better sustainable stability at a lower concentration than P123 due to the moderate positive potential value (39.43±3.45 mV) and the lower critical micelle concentration (0.036 mg/ml). Dual drugs were loaded with CP-FA nanogels via self-assembly by the hydrophobic interaction between both hydrophobic therapeutic compounds (PTX and Cur) and the hydrophobic segment of the P123 copolymer. The high hydrophobicity of the segment induced a great loading efficacy of up to 98.63±0.42 of PTX and 97.82±0.48 of Cur. In addition, the CP-FA nanogels exposed superior effects in a controlled release of these encapsulated therapeutic compounds for a long period of time. The anticancer activity of the dual-drug delivery system was evaluated using human breast cancer cell lines (MCF-7) via the IC50 value to compare with the PTX-loading CP-FA nanogel. The obtained results suggested that CP-FA/PTX-Cur displayed a remarkable improvement in anticancer activity at an IC50 value of 5.74±0.23 nM which was higher than that of CP-FA/PTX (IC50=8.20±1.41 nM) due to the synergistic effect of both PTX and Cur. Thereby, a dual-drug delivery-system-based CP-FA of PTX and Cur has been proposed as a promising candidate in cancer therapy.