Winter Evelyn, Pizzol Carine Dal, Locatelli Claudriana, Silva Adny H, Conte Aline, Chiaradia-Delatorre Louise D, Nunes Ricardo J, Yunes Rosendo A, Creckzynski-Pasa Tânia B
Department of Pharmaceutical Sciences, Federal University of Santa Catarina, P.O. Box 476, Florianópolis, SC 88040-900, Brazil.
Department of Pharmacy, University of West of Santa Catarina, Videira, SC 89560-000, Brazil.
Int J Environ Res Public Health. 2014 Sep 26;11(10):10016-35. doi: 10.3390/ijerph111010016.
Several obstacles are encountered in conventional chemotherapy, such as drug toxicity and poor stability. Nanotechnology is envisioned as a strategy to overcome these effects and to improve anticancer therapy. Nanoemulsions comprise submicron emulsions composed of biocompatible lipids, and present a large surface area revealing interesting physical properties. Chalcones are flavonoid precursors, and have been studied as cytotoxic drugs for leukemia cells that induce cell death by different apoptosis pathways. In this study, we encapsulated chalcones in a nanoemulsion and compared their effect with the respective free compounds in leukemia and in non-tumoral cell lines, as well as in an in vivo model. Free and loaded-nanoemulsion chalcones induced a similar anti-leukemic effect. Free chalcones induced higher toxicity in VERO cells than chalcones-loaded nanoemulsions. Similar results were observed in vivo. Free chalcones induced a reduction in weight gain and liver injuries, evidenced by oxidative stress, as well as an inflammatory response. Considering the high toxicity and the side effects induced generally by all cancer chemotherapies, nanotechnology provides some options for improving patients' life quality and/or increasing survival rates.
传统化疗面临若干障碍，如药物毒性和稳定性差。纳米技术被视为克服这些影响并改善抗癌治疗的一种策略。纳米乳剂由生物相容性脂质构成的亚微米乳剂组成，具有较大的表面积，展现出有趣的物理性质。查耳酮是类黄酮前体，已作为细胞毒性药物用于白血病细胞研究，其通过不同凋亡途径诱导细胞死亡。在本研究中，我们将查耳酮包封于纳米乳剂中，并比较它们与各自游离化合物对白血病细胞系和非肿瘤细胞系以及体内模型的作用。游离查耳酮和负载纳米乳剂的查耳酮诱导了相似的抗白血病效应。游离查耳酮对VERO细胞的毒性高于负载查耳酮的纳米乳剂。在体内也观察到了类似结果。游离查耳酮导致体重增加减少和肝损伤，表现为氧化应激以及炎症反应。考虑到所有癌症化疗通常都会引起的高毒性和副作用，纳米技术为提高患者生活质量和/或提高生存率提供了一些选择。
