Background: Artemisinin is a sesquiterpene lactone chemical extract from Artemisia annua, is poorly resolvable in water and a fast-acting blood active in treating the acute attack of malaria. Methods: Artemisinin was encapsulated within mPEG-PCL micelles with a single-step nano-precipitation method, leading to formation of ART/ mPEG-PCL micelles. mPEG-PCL copolymers was characterized in vitro by HNMR, FTIR and DSC techniques. Copolymers with artemisinin were self-assembled into micelles in aqueous solution. The consequential micelles were further characterized by various techniques such as DLS and AFM. Results: The results exhibited the successful formation of spherical artemisinin-loaded micelles. The artemisinin-loaded micelles showed high loading efficiency. The encapsulation efficiency of artemisinin was 63±2.31%. In vitro release of artemisinin from artemisinin-entrapped micelles followed remarkably sustained release profile. Conclusion: The results indicated that the successful formulation of artemisinin loaded mPEG-PCL micelles can improve the drug delivery of artemisinin. The results showed that nanomicelles can be promising drug delivery systems for sustaining release of artemisinin.
Introduction: Due to the side effects of drugs, the development of nanoscale drug delivery systems has led to a significant improvement in medicinal therapies due to drug pharmacokinetics changes, decreased toxicity, and increased half-life of the drug. This study aimed to synthesize tamoxifen (TMX)-loaded L-lysine coated magnetic iron oxide nanoparticles as a nano-carrier to investigate its cytotoxic effects and anti-cancer properties against MCF-7 cancer cells. Methods: Magnetic Fe3O4 nanoparticles were synthesized and coated with L-lysine (F-Lys NPs). Then, TMX was loaded onto these NPs. The characteristics of synthesized nanoparticles (F-Lys-TMX NPs) were evaluated by X-ray diffraction (XRD), Fourier-transform infrared spectroscopy (FTIR), scanning electron microscopy (SEM), transmission electron microscopy (TEM), dynamic light scattering (DLS), differential scanning calorimetry (DSC), vibrating sample magnetometer (VSM), and thermogravimetric analysis (TGA). The drug release was analyzed at pH 5.8 and pH 7.4. The MCF-7 cells were exposed to F-Lys-TMX NPs, F-Lys NPs, and TMX for 24, 48, and 72 hours. To evaluate the cytotoxic potential of designed nanoparticles, MTT and apoptosis assays, real-time PCR, and cell cycle analysis was carried out. Results: The F-Lys-TMX NPs had spherical morphology with a size ranging from 9 to 30 nm. By increasing the nanoparticles concentration and treatment time, more cell proliferation inhibition and apoptosis induction were observed in F-Lys-TMX NPs-treated cells compared to the TMX. The expression levels of ERBB2, cyclin D1, and cyclin E genes were down-regulated and expression levels of the caspase-3 and caspase-9 genes were up-regulated. Studies on the drug release revealed a slow and controlled pH-dependent release of the nanoparticles. Cell cycle analysis indicated that F-Lys-TMX NPs could arrest the cells at the G0/G1 phase. Conclusion: The findings suggest that F-Lys-TMX NPs are more effective and have the potential for cell proliferation inhibition and apoptosis induction compared to the TMX. Hence, F-Lys-TMX NPs can be considered as an anti-cancer agent against MCF-7 breast cancer cells.
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