Perez-Ruiz Adriana Guadalupe, Ganem Adriana, Olivares-Corichi Ivonne María, García-Sánchez José Rubén
Sección de Estudios de Posgrado e Investigación, Escuela Superior de Medicina del Instituto Politécnico Nacional Ciudad de México Mexico
Division de Estudios de Posgrado (Tecnología Farmacéutica), Facultad de Estudios Superiores Cuautitlán, Universidad Nacional Autónoma de Mexico Cuautitlán Izcalli Estado de Mexico Mexico.
RSC Adv. 2018 Oct 10;8(61):34773-34782. doi: 10.1039/c8ra06327c.
Natural compounds such as (-)-epicatechin show a variety of biological properties including anticancer activity. Nonetheless, (-)-epicatechin's therapeutic application is limited due to its low water solubility and sensitivity to oxygen and light. Additionally, previous studies have reported that the encapsulation of flavonoids in nanoparticles might generate stable deliverable forms, which improves the availability and solubility of the bioactive compounds. The aims of this study were to generate (-)-epicatechin-loaded lecithin-chitosan nanoparticles (EC-LCT-NPs) by molecular self-assembly and to assess their cytotoxic potential against breast cancer cells. Various parameters were measured to characterize the EC-LCT-NPs including size, polydispersity index (PdI), zeta potential, morphology and entrapment efficiency. The results showed that the mean particle size of the EC-CLT-NPs was 159 ± 2.23 nm (PdI, 0.189), and the loading and entrapment efficiencies of (-)-epicatechin were 3.42 ± 0.85% and 56.1 ± 3.9%, respectively. The cytotoxic effect of the EC-CLT-NPs was greater than that of free (-)-epicatechin on breast cancer cell lines (MCF-7, MDA-MB-231, MDA-MB-436 and SK-Br3). Indeed, EC-LCT-NPs showed an IC that was four-fold lower (85 μM) than free (-)-epicatechin (350 μM) and showed selectivity to cancerous cells. This study demonstrated that encapsulating (-)-epicatechin into lecithin-chitosan nanoparticles opens new options for breast cancer treatment.
诸如(-)-表儿茶素之类的天然化合物具有多种生物学特性,包括抗癌活性。尽管如此,(-)-表儿茶素的治疗应用因其低水溶性以及对氧气和光的敏感性而受到限制。此外,先前的研究报道,将黄酮类化合物包裹在纳米颗粒中可能会产生稳定的可递送形式,这提高了生物活性化合物的利用率和溶解度。本研究的目的是通过分子自组装生成负载(-)-表儿茶素的卵磷脂-壳聚糖纳米颗粒(EC-LCT-NPs),并评估其对乳腺癌细胞的细胞毒性潜力。测量了各种参数以表征EC-LCT-NPs,包括尺寸、多分散指数(PdI)、zeta电位、形态和包封率。结果表明,EC-CLT-NPs的平均粒径为159±2.23nm(PdI,0.189),(-)-表儿茶素的负载率和包封率分别为3.42±0.85%和56.1±3.9%。EC-CLT-NPs对乳腺癌细胞系(MCF-7、MDA-MB-231、MDA-MB-436和SK-Br3)的细胞毒性作用大于游离(-)-表儿茶素。实际上,EC-LCT-NPs的半数抑制浓度(IC)比游离(-)-表儿茶素(350μM)低四倍(85μM),并且对癌细胞具有选择性。本研究表明,将(-)-表儿茶素包裹在卵磷脂-壳聚糖纳米颗粒中为乳腺癌治疗开辟了新的途径。