Department of Chemistry, Faculty of Science and Arts, Natural Products and Drug Research Laboratory, Canakkale Onsekiz Mart University, Canakkale, Turkey.
Department of Experimental Therapeutics, The University of Texas MD Anderson Cancer Center, 1515 Holcombe Boulevard, Unit 422, Houston, Texas, 77030, USA.
Pharm Res. 2020 Mar 4;37(3):63. doi: 10.1007/s11095-020-2774-5.
To evalauted natural polymeric biomaterials including hyaluronic acid (HA) and its copolymeric form HA:Suc nanoparticles (NPs) as drug carrier systems for delivery of hydrophobic small molecule kinase EF2-kinase inhibitor in breast and pancreatic cancer cells.
In vitro cellular uptake studies of Rhodamine 6G labaled HA:Suc nanoparticles were evaluated by using flow cytometry analysis and fluorescent microscopy in breast (MDA-MB-231 and MDA-MB-436) and pancreatic cancer cells (PANC-1 and MiaPaca-2). Besides, in vitro release study of compound A (an EF2-kinase inhibitor) as a model hydrophobic drug was performed in the cancer cells.
These biological evaluation studies indicated that HA and HA:Suc NPs provided a highly effective delivery of compound A were into breast and pancreatic cancer cells, leading to significant inhibition of cell proliferation and colony formation of breast and pancreatic cancer cells.
HA-sucrose NPs incorporating an EF2-Kinase inhibitor demonstrate significant biologic activity in breast and pancreatic cancer cells. This is the first study that shows natural polymeric drug carriers succesfully deliver a hydrofobic cancer drug into cancer cells. Graphical Abstract Nanoparticles based on HA:Suc are effective in delivering hydrofobic cancer drugs in breast and pancreatic cancers.
评估包括透明质酸（HA）及其共聚物形式的 HA：蔗糖纳米粒子（NPs）在内的天然聚合物生物材料作为药物载体系统，用于在乳腺癌和胰腺癌细胞中递送疏水分子激酶 EF2-激酶抑制剂。
通过流式细胞术分析和荧光显微镜评估 Rhodamine 6G 标记的 HA：蔗糖纳米粒子在乳腺癌（MDA-MB-231 和 MDA-MB-436）和胰腺癌细胞（PANC-1 和 MiaPaca-2）中的体外细胞摄取研究。此外，在癌细胞中进行了作为模型疏水性药物的化合物 A（EF2-激酶抑制剂）的体外释放研究。
这些生物学评价研究表明，HA 和 HA：蔗糖 NPs 能够非常有效地将化合物 A 递送至乳腺癌和胰腺癌细胞，从而显著抑制乳腺癌和胰腺癌细胞的增殖和集落形成。
包含 EF2-激酶抑制剂的 HA-蔗糖 NPs 在乳腺癌和胰腺癌细胞中表现出显著的生物学活性。这是第一项表明天然聚合物药物载体成功将疏水性癌症药物递送至癌细胞中的研究。
基于 HA：蔗糖的纳米粒子可有效递送至乳腺癌和胰腺癌中的疏水性癌症药物。
