Department of Biological Sciences, Faculty of Pure and Applied Sciences, University of Cyprus, Nicosia, Cyprus.
Department of Electrical and Computer Engineering University of Cyprus, Nicosia, Cyprus.
Nanotheranostics. 2021 Jan 1;5(1):113-124. doi: 10.7150/ntno.51955. eCollection 2021.
Treatment of breast cancer underwent extensive progress in recent years with molecularly targeted therapies. However, non-specific pharmaceutical approaches (chemotherapy) persist, inducing severe side-effects. Phytochemicals provide a promising alternative for breast cancer prevention and treatment. Specifically, resveratrol (res) is a plant-derived polyphenolic phytoalexin with potent biological activity but displays poor water solubility, limiting its clinical use. Here we have developed a strategy for delivering res using a newly synthesized nano-carrier with the potential for both diagnosis and treatment. Res-loaded nanoparticles were synthesized by the emulsion method using Pluronic F127 block copolymer and Vitamin E-TPGS. Nanoparticle characterization was performed by SEM and tunable resistive pulse sensing. Encapsulation Efficiency (EE%) and Drug Loading (DL%) content were determined by analysis of the supernatant during synthesis. Nanoparticle uptake kinetics in breast cancer cell lines MCF-7 and MDA-MB-231 as well as in MCF-10A breast epithelial cells were evaluated by flow cytometry and the effects of res on cell viability via MTT assay. Res-loaded nanoparticles with spherical shape and a dominant size of 179±22 nm were produced. Res was loaded with high EE of 73±0.9% and DL content of 6.2±0.1%. Flow cytometry revealed higher uptake efficiency in breast cancer cells compared to the control. An MTT assay showed that res-loaded nanoparticles reduced the viability of breast cancer cells with no effect on the control cells. These results demonstrate that the newly synthesized nanoparticle is a good model for the encapsulation of hydrophobic drugs. Additionally, the nanoparticle delivers a natural compound and is highly effective and selective against breast cancer cells rendering this type of nanoparticle an excellent candidate for diagnosis and therapy of difficult to treat mammary malignancies.
近年来,随着分子靶向疗法的发展,乳腺癌的治疗取得了广泛的进展。然而,非特异性药物治疗(化疗)仍然存在,并引起严重的副作用。植物化学物质为乳腺癌的预防和治疗提供了有希望的替代方法。具体来说,白藜芦醇(res)是一种具有强大生物活性的植物源性多酚植物抗毒素,但水溶性差,限制了其临床应用。在这里,我们开发了一种使用新合成的纳米载体递送 res 的策略,该载体具有诊断和治疗的双重潜力。通过乳液法使用 Pluronic F127 嵌段共聚物和维生素 E-TPGS 合成了载有 res 的纳米粒子。通过 SEM 和可调电阻脉冲感应对纳米粒子进行了表征。通过分析合成过程中的上清液确定了包封效率(EE%)和药物负载(DL%)含量。通过流式细胞术评估了载有 res 的纳米粒子在乳腺癌细胞系 MCF-7 和 MDA-MB-231 以及乳腺上皮细胞 MCF-10A 中的摄取动力学,并通过 MTT 测定法评估了 res 对细胞活力的影响。以球形形状和 179±22nm 的主要粒径生产出载有 res 的纳米粒子。Res 的 EE 为 73±0.9%,DL 含量为 6.2±0.1%。流式细胞术显示与对照相比,乳腺癌细胞的摄取效率更高。MTT 测定表明,载有 res 的纳米粒子降低了乳腺癌细胞的活力,而对对照细胞没有影响。这些结果表明,新合成的纳米粒子是包封疏水性药物的良好模型。此外,纳米粒子递送天然化合物,对乳腺癌细胞具有高度的有效性和选择性,使这种类型的纳米粒子成为治疗难以治疗的乳腺恶性肿瘤的诊断和治疗的优秀候选者。