Purpose: Among the potent anticancer agents, d,l-sulforaphane (SF) is very effective against many different types of cancer cells. Its clinical application is restricted because of its hydrophobicity, low gastrointestinal absorption and poor bioavailability. In the present study, a reliable micellar delivery system using monomethoxypoly (ethylene glycol)–poly (ɛ-caprolactone) (mPEG–PCL) was established. The encapsulation of SF inside mPEG–PCL as a nano-carrier was established and the cytotoxicity assay against human breast cancer cell line was evaluated. Methods: In this study, SF was encapsulated within mPEG–PCL micelles through a single-step nano-precipitation method, leading to creation of SF-loaded mPEG–PCL (SF/mPEG–PCL) micelles. Di-block mPEG–PCL copolymers were synthesized and used to prepare micelles. MPEG-PCL copolymer was characterized by HNMR, FTIR, differential scanning calorimetry and gel permeation chromatography techniques. Characterization, stability of micelles, the particle size and morphology were determined. The release profile of the SF from the micelles which prepared by the drug-loaded copolymer, was evaluated. The cytotoxicity of free SF, mPEG–PCL and SF-loaded mPEG–PCL micelles was compared with each other by performing MTT assay of the treated MCF-7 cell line. Expression levels of BCL-2, MMP-9, BCL-XL, BAK, BAX and GAPDH (endogenous gene) as control were quantified by real time PCR. To evaluate the apoptotic effects of Free SF compared with SF-loaded mPEG–PCL micelles, flow cytometry analysis was done using the annexin V-FITC apoptosis detection kit. Results: Our studies resulted in a successful establishment of uniformity and spherical SF-loaded mPEG–PCL micelles. The encapsulation efficiency of SF was 86 ± 1.58%. The results of atomic force microscopy revealed that the micelles have spherical shapes with size of 107 nm. In vitro release of SF from SF-entrapped micelles was remarkably sustained. The mPEG–PCL micelle showed little cytotoxicity in the case of MCF-7 cell line with concentration up to 1.5 mg/ml, whereas the SF-loaded mPEG–PCL micelles at all concentrations significantly was cytotoxic in the case of MCF-7 cell line. Finally, real-time PCR and flow cytometry were used to demonstrate that the SF-loaded mPEG–PCL could be efficiently inducing apoptosis in MCF-7 cell line. Conclusion: We achieved to a successful formulation of SF-loaded m-PEG/PCL micelles in this study. Based on the cytotoxicity results of mPEG–PCL micelles against human breast cancer cell line (MCF-7) in this study, it suggested that SF/mPEG–PCL micelles can be an effective breast cancer treatment strategy in the future.

Methotrexate (MTX), a stoichiometric inhibitor of dihydrofolate reductase enzyme, is a chemotherapeutic agent for treating a diversity of neoplasms. In this study, we design and developed a new formulation of MTX that serves as drug carrier and examined its cytotoxic effect in vitro. This target drug delivery system is dependent on the release of the MTX within the lysosomal compartment. The iron oxide magnetic nanoparticles (IONPs) were first surface-coated with L-lysine and subsequently conjugated with MTX through amidation between the carboxylic acid end groups on MTX and the amine groups on the IONPs surface. MTX-conjugated L-lysine coated IONPs (F-Lys-MTX NPs) was characterized by X-ray diffraction, thermogravimetric analysis, differential scanning calorimetry, Fourier transform infrared spectroscopy, vibrating sample magnetometer, and transmission electron microscopy techniques. The cytotoxicity of the void of MTX and F-Lys-MTX NPs were compared to each other by MTT assay of the treated MCF-7 cell lines. The results showed that the ζ-potential of F-Lys-MTX NPs was about −5.49 mV and the average size was 43.72 ± 4.73 nm. Model studies exhibited the release of MTX via peptide bond cleavage in the presence of proteinase K and at low pH. These studies specify that F-Lys-MTX NPs have a very remarkable anticancer effect, for breast cancer cell lines.

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.