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Artemisinin (ART) is a natural anti-malarial sesquiterpene lactone with anticancer properties, but its application is limited because of its low water solubility. To increase the bioavailability and water solubility of ART, we synthesized three series of poly (ɛ-caprolactone)-poly (ethylene glycol)-poly (ɛ-caprolactone) (PCL-PEG-PCL) tri-block copolymers. The structure of the copolymers was characterized by HNMR, FTIR, DSC and GPC techniques. ART was encapsulated inside micelles by a nanoprecipitation method which leading to the formation of ART/PCL-PEG-PCL micelles. The obtained micelles were characterized by DLS and AFM technique. The results showed that the average size of micelles was about 83.22 nm. ART was encapsulated into PCL-PEG-PCL micelles with encapsulation efficacy of 89.23 ± 1.41%. In vivo results demonstrated that this formulation significantly increased drug accumulation in tumours. Pharmacokinetic study in rats revealed that in vivo drug exposure of ART was significantly increased and prolonged by intravenously administering ART-loaded micelles when compared with the same dose of free ART. The MTT assay showed that bare PCL-PEG-PCL micelles is non-toxic to MCF7 and 4T1 cancer cell lines whereas the ART/PCL-PEG-PCL micelles showed a specific toxicity to both cancer cell lines. Therefore, the polymeric micellar formulation of ART based copolymer could provide a desirable process for ART delivery.

We report the synthesis of iron oxide magnetic nanoparticles (IONPs) coated with various natural amino acids (AAs) using a one‐pot reaction in an aqueous medium. Several AAs, which contained hydrophilic and hydrophobic groups, were selected to study their effects on size, morphology and toxicity of IONPs. Functionalized IONPs were characterized using X‐ray diffraction, differential scanning calorimetry, thermogravimetric analysis, Fourier transform infrared spectroscopy, and scanning and transmission electron microscopies. Furthermore, vibrating sample magnetometry analysis shows these nanoparticles have excellent magnetic properties. Cellular toxicity of IONPs was also investigated on HFF2 cell lines. The AA‐coated IONPs are non‐toxic and biocompatible. Natural AA‐coated IONPs show a potential for their development in in vitro and in vivo biomedical fields due to their non‐toxicity, good ζ‐potential and related small size and narrow size distribution.

A reliable and efficient drug delivery system using PCL-PEG-PCL copolymers was established for the anti-cancer compound sulforaphane (SF) in this study. Encapsulated SF by PCL-PEG-PCL nanoparticles led to formation of SF-loaded PCL-PEG-PCL micelles. Micelles characterization and stability, the particle size and their morphology were determined by DLS and AFM. The loading efficiency of SF was 19.33 ± 1.28%. The results of AFM showed that the micelles had spherical shapes with the size of 107 nm. In vitro release of SF from SF-entrapped micelles was remarkably sustained. The cytotoxicity of free SF, PCL-PEG-PCL and SF/PCL-PEG-PCL micelles was analysis by MTT colorimetric assay on MCF-7, 4T1 and MCF10A cell lines. Expression levels of BCL-2, PARP, COX-2, Caspase-9 and ACTB genes were quantified by real-time PCR. Flow cytometry analysis was performed using the Annexin V-FITC Apoptosis Detection Kit to evaluate the apoptotic effects of free SF compared with SF/PCL-PEG-PCL micelles. Study of the in vivo pharmacokinetics of the SF-loaded micelles was carried out on SF-loaded PCL-PEG-PCL micelles in comparison with free SF. The results of in vivo experiments indicated that the SF loaded micelles significantly reduced the tumor size. In vivo results showed that the multiple injections of SF-loaded micelles could prolong the circulation period and increase the therapeutic efficacy of SF. Also, in comparison with the free-SF solution, encapsulation of the SF in micelles increased the mean residence time from 0.5 to 4 h and the area under the concentration-time curve up to 50 folds.

In this study, we have achieved to provide an efficient method for production of iron oxide magnetic nanoparticles (MNPs) with arginine capping using in situ and one-pot co-precipitation method. As a novel drug delivery system, methotrexate (MTX) was conjugated to the obtained nanoparticles. These MNPs conjugate can potentially use in controlled drug delivery as carrier, and in magnetic resonance imaging as a contrast agent.Also, these nanoparticles can serve as a target in cancer therapy and diagnosis. These MNPs were covalently bond with MTX and can target the majority of cancer cells that their surfaces overexpressed by folate receptors. These conjugated nanoparticles were obtained through amide bond between the amine groups on their surface and the carboxylic acid end groups on MTX due to being functionalized with arginine. MTX was cleaved from nanoparticles according to drug release experiments in the presence of protease-like lysosomal conditions. Fe-Arg-MTX was characterized by transmission electron microscopes, dynamic light scattering, thermogravimetric analysis, differential scanning calorimetry, X-ray diffraction, and Fourier transform infrared spectroscopy.Furthermore, vibrating sample magnetometry analysis showed excellent magnetic properties of them. The average particle size of Fe-Arg-MTX was approximately 27 nm. The result revealed that the bare nanoparticles have no cytotoxicity against MCF-7, 4T1, and HFF-2 cell lines. Hemolysis assay showed that these nanoparticles are biocompatible.Regarding the research success, an efficient technique can be presented for drug delivery and controlled release and for studying cancer-fighting in alive creature's bodies. K E Y W O R D Santicancer, arginine, drug conjugated, methotrexate, paramagnetic nanoparticle

Synchronous chemotherapy and radiotherapy, termed chemoradiation therapy, is now an important standard regime for synergistic cancer treatment. For such treatment, nanoparticles can serve as improved carriers of chemotherapeutics into tumors and as better radiosensitizers for localized radiotherapy. Herein, we designed a Schottky-type theranostic heterostructure, Bi 2 S 3 –Au, with deep level defects (DLDs) in Bi 2 S 3 as a nano-radiosensitizer and CT imaging contrast agent which can generate reactive free radicals to initiate DNA damage within tumor cells under X-ray irradiation. Methotrexate (MTX) was conjugated onto the Bi 2 S 3 –Au nanoparticles as a chemotherapeutic agent showing enzymatic stimuli-responsive release behavior. The designed hybrid system also contained curcumin (CUR), which cannot only serve as a nutritional supplement for chemotherapy, but also can play an important role in the radioprotection of normal cells. Impressively, this combined one-dose chemoradiation therapeutic injection of co-drug loaded bimetallic multifunctional theranostic nanoparticles with a one-time clinical X-ray irradiation, completely eradicated tumors in mice after approximately 20 days after irradiation showing extremely effective anticancer efficacy which should be further studied for numerous anti-cancer applications.

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In this study we reported the synthesis of L-phenyl alanine (Phe) & L-tyrosine (Tyr) Natural Amino acids coated iron oxide magnetic nanoparticles under one-pot and in situ reaction. Functionalized iron oxide magnetic nanoparticles were characterized by X-ray diffraction (XRD), differential scanning calorimetry (DSC), thermogravimetric analysis (TGA), Vibrating Sample Magnetometer (VSM), Fourier transform infrared spectroscopy (FTIR), Scanning electron microscopy (SEM) and Transmission electron microscopy (TEM) techniques. Cellular toxicity of amino acids coated iron oxide magnetic nanoparticles was also investigated on HEK-293 cell lines. Additionally, a hemolysis test of as prepared magnetic nanoparticles were performed. It was found that the synthesized Phe and Tyr coated magnetic nanoparticles (F@Phe NPs and F@Tyr NPs) were spherical in shape with an average size less than 25 nm, also the saturation magnetization (Ms) of the F@Phe NPs and F@Tyr NPs were about 30.02 and 58.23 emu/g, respectively, which was lower than those of bare FeO. The TGA results show that apart from this weight loss, the coated sample shows a weight loss of 5.48, and 6.88% respectively corresponding to loss of Tyr, and Phe which is coated on the FeO nanoparticles. At a high concentration, less than 2.92 and 3.13% hemolytic activity were observed for F@Phe NPs and F@Tyr NPs, respectively. The F@Phe NPs and F@Tyr NPs show the possibility of using this nanoparticles in the development of in vitro and in vivo pharmaceutical and biomedical fields due to do not possess a toxic effect, good ζ-potential and related small and narrow size distribution.