Hajipour Hamed, Hamishehkar Hamed, Nazari Soltan Ahmad Saeed, Barghi Siamak, Maroufi Nazila Fathi, Taheri Ramezan Ali
a Student Research Committee and Department of Reproductive Biology, Faculty of Advanced Medical Sciences , Tabriz University of Medical Sciences , Tabriz , Iran.
b Nanobiotechnology Research Center , Baqiyatallah University of Medical Sciences , Tehran , Iran.
Artif Cells Nanomed Biotechnol. 2018;46(sup1):283-292. doi: 10.1080/21691401.2017.1423493. Epub 2018 Jan 8.
The global burden of cancer have encouraged oncologists to develop novel strategies for treatment. Present study was proposed to develop Arginyl-glycyl-aspartic acid (RGD)-containing nanostructured lipid carriers (NLC) as a delivery system for improving the anticancer capability of epigallocatechin gallate (EGCG) on breast cancer cell line by attaching to integrin superfamily on cancer cells. For this purpose, RGD-containing EGCG-loaded NLC were prepared by hot homogenization technique and characterized by different techniques. Then, cytotoxic and apoptotic effects of prepared nanoparticles and their uptake into cells was evaluated. As results, the nanoparticles with particle size of 85 nm, zeta potential of -21 mV, encapsulation of 83% were prepared. Cytotoxicity and apoptosis experiments demonstrated that EGCG-loaded NLC-RGD possessed greatest apoptotic activity. Furthermore, it has been shown that, EGCG-loaded NLC-RGD causes cell cycle arresting more effective than EGCG. Therefore, loading EGCG into NLC-RGD make it more effective in both targeting and accumulation into tumour cells, which results from specialized uptake mechanism by adhesion to αvβ3 integrin. The results strengthen our hope that loading EGCG into RGD-containing NLC could possibly overcome the therapeutic limitations of EGCG and make it more effective in cancer therapy.
癌症的全球负担促使肿瘤学家开发新的治疗策略。本研究旨在开发含精氨酰-甘氨酰-天冬氨酸（RGD）的纳米结构脂质载体（NLC）作为一种递送系统，通过与癌细胞上的整合素超家族结合来提高表没食子儿茶素没食子酸酯（EGCG）对乳腺癌细胞系的抗癌能力。为此，采用热均质技术制备了含RGD的载EGCG的NLC，并通过不同技术对其进行表征。然后，评估了所制备纳米颗粒的细胞毒性和凋亡作用及其对细胞的摄取情况。结果制备出了粒径为85 nm、zeta电位为-21 mV、包封率为83%的纳米颗粒。细胞毒性和凋亡实验表明载EGCG的NLC-RGD具有最大的凋亡活性。此外，研究表明载EGCG的NLC-RGD比EGCG更有效地导致细胞周期停滞。因此，将EGCG负载到NLC-RGD中使其在靶向和积聚到肿瘤细胞方面更有效，这是由于通过与αvβ3整合素粘附的特殊摄取机制所致。这些结果增强了我们的希望，即将EGCG负载到含RGD的NLC中可能克服EGCG的治疗局限性并使其在癌症治疗中更有效。
