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Deferasirox-loaded polymeric micelles as nanoformulated iron chelating chemotherapy of prostate cancer

机译：负载地拉罗司的聚合物胶束作为前列腺癌的纳米铁螯合化学疗法

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Nowadays, conventional chemotherapy is commonly used in many cancers and support for other cancer therapies to improve the success rate of treatment. However, the conventional chemotherapy has many severe side effects. Thus, polymers and nanotechnology are applied to develop drug delivery systems and to increase the properties of anti-cancer drug including reduction of side effect. Many reports show that the cancer cells express higher iron level therefore inhibiting iron metabolism in cancer cells is a novel strategy to treat cancer. Generally, iron chelator used to reduce iron overload in the thalassemia patients. In this experiment, iron chelator, deferasirox (Dei) was used as anticancer drug that is trapped iron in cancer cells leading to antiproliferation of cancer cells. Deferasirox was loaded into PEG-A-PCL (MW of PEG = 5.0 kDa, MW of PCL = 5.0 kDa) polymeric micelles by the solvent evaporation method. The hydrodynamic diameter of Def-loaded micelles was measured. Released studies of Def were monitored in PBS pH 7.4. The drug loading content (DLC) and drug loading efficiency (EE) were determined. Def-loaded micelles was incubated with PC-3 cells for 72 h and viability of PC-3 was determined by MTT assay. The result shows that ICS0 of free Def was 8.74 μM and IC50 of Def-loaded Micelles was 12.85 μM. This suggests that the Def and Def-loaded micelles were able to trap a free iron in cytoplasm and induce antiproliferation of PC-3 cells that is an alternative technique to kill cancer cells.
机译：如今，常规化学疗法已广泛用于许多癌症中，并支持其他癌症疗法以提高治疗成功率。然而，常规化学疗法具有许多严重的副作用。因此，聚合物和纳米技术被用于开发药物递送系统并增加抗癌药的性能，包括减少副作用。许多报道表明癌细胞表达较高的铁水平，因此抑制癌细胞中的铁代谢是治疗癌症的新策略。通常，铁螯合剂用于减少地中海贫血患者的铁超负荷。在该实验中，铁螯合剂Deferasirox（Dei）被用作抗癌药物，该药物将铁捕获在癌细胞中，从而导致癌细胞的抗增殖。通过溶剂蒸发法将地拉罗司装载到PEG-A-PCL（PEG的MW = 5.0 kDa，PCL的MW = 5.0 kDa）聚合物胶束中。测量了Def负载胶束的流体动力学直径。在PBS pH 7.4中监测Def释放的研究。确定了载药量（DLC）和载药效率（EE）。脱胶的胶束与PC-3细胞孵育72小时，并通过MTT法测定PC-3的活力。结果表明，游离Def的ICS0为8.74μM，Def负载胶束的IC50为12.85μM。这表明Def和Def加载的胶束能够捕获细胞质中的游离铁并诱导PC-3细胞的抗增殖，这是杀死癌细胞的另一种技术。

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