Post-Graduation Program in Health Sciences, Faculty of Medical Sciences, Federal University of Mato Grosso, Cuiabá, Brazil.
Post-Graduation Program in Health Sciences, Federal University of Mato Grosso, Sinop, Brazil.
Pharm Dev Technol. 2022 Oct;27(8):892-903. doi: 10.1080/10837450.2022.2128819. Epub 2022 Oct 3.
Glioblastomas are tumors that present a high mortality rate. Artemether (ART) is a lactone with antitumor properties, demonstrating low bioavailability and water solubility. In the present study, we developed lipid-core nanocapsules (LNC) containing pequi oil ( Cambess) as the oily core for ART-loaded LNCs (LNC) and evaluated their effect on human glioblastoma cells (U-87 MG). LNCs were developed by interfacial deposition of a preformed polymer, followed by physicochemical characterization. LNC revealed a diameter of 0.216 µm, polydispersity index of 0.161, zeta potential of -12.0 mV, and a pH of 5.53. Furthermore, mitochondrial viability, proliferation, total antioxidant status, and antioxidant enzyme activity were evaluated. ART reduced cell viability after 24 h and proliferation after 48 h of treatment at concentrations equal to or above 40 µg . mL. LNC, at 1.25 µg . mL, reduced these parameters after 24 h of treatment. Furthermore, superoxide dismutase (SOD) activity was elevated, while glutathione reductase (GR) activity was reduced. These findings suggest that ART loaded into LNC may be a promising alternative to improve its pharmacological action and possible application as a therapeutic agent for glioblastoma.
胶质母细胞瘤是一种死亡率很高的肿瘤。青蒿琥酯(ART)是一种具有抗肿瘤特性的内酯,但其生物利用度和水溶性较低。在本研究中,我们开发了含有 pequi 油(Cambess)作为油性核心的脂质核纳米胶囊(LNC),用于载 ART 的 LNC(LNC),并评估了其对人胶质母细胞瘤细胞(U-87 MG)的作用。LNC 通过界面沉积预先形成的聚合物来开发,然后进行理化特性表征。LNC 的直径为 0.216 µm,多分散指数为 0.161,zeta 电位为-12.0 mV,pH 值为 5.53。此外,还评估了线粒体活力、增殖、总抗氧化状态和抗氧化酶活性。ART 在浓度等于或高于 40 µg·mL 时,在 24 h 后降低细胞活力,在 48 h 后降低增殖。LNC 在 1.25 µg·mL 时,在 24 h 后降低这些参数。此外,超氧化物歧化酶(SOD)活性升高,而谷胱甘肽还原酶(GR)活性降低。这些发现表明,负载到 LNC 中的 ART 可能是改善其药理作用的一种有前途的替代方法,并有希望作为治疗胶质母细胞瘤的药物。