Alasvand Neda, Saeidifar Maryam, Saboury Ali Akbar, Mozafari Masoud
Bioengineering Research Group, Nanotechnology and Advanced Materials Department, Materials and Energy Research Center (MERC), P.O. Box 14155-4777, Tehran, Iran.
Institute of Biochemistry and Biophysics (IBB), University of Tehran, Tehran, Iran.
IET Nanobiotechnol. 2017 Aug;11(5):591-596. doi: 10.1049/iet-nbt.2016.0164.
Over the past few years, there have been several attempts to deliver anticancer drugs into the body. It has been shown that compared to other available carriers, colloidal gelatin nanoparticles (CGNPs) have distinct properties due to their exceptional physico-chemical and biological characteristics. In this study, a novel water-soluble palladium (II) anticancer complex was first synthesised, and then loaded into CGNPs. The CGNPs were synthesised through a two-step desolvation method with an average particle size of 378 nm. After confirming the stability of the drug in the nanoparticles, the drug-loaded CGNPs were tested for in vitro cytotoxicity against human breast cancer cells. The results showed that the average drug encapsulating efficiency and drug loading of CGNPs were 64 and 10 ± 2.1% (w/w), respectively. There was a slight shift to higher values of cumulative release, when the samples were tested in lower pH values. In addition, the in vitro cytotoxicity test indicated that the number of growing cells significantly decreased after 48 h in the presence of different concentrations of drug. The results also demonstrated that the released drug could bind to DNA by a static mechanism at low concentrations (0.57 µM) on the basis of hydrophobic and hydrogen binding interactions.
在过去几年中,人们多次尝试将抗癌药物输送到体内。研究表明,与其他可用载体相比,胶体明胶纳米颗粒(CGNPs)因其特殊的物理化学和生物学特性而具有独特的性质。在本研究中,首先合成了一种新型水溶性钯(II)抗癌配合物,然后将其负载到CGNPs中。通过两步去溶剂化方法合成了CGNPs,平均粒径为378 nm。在确认药物在纳米颗粒中的稳定性后,对载药CGNPs进行了对人乳腺癌细胞的体外细胞毒性测试。结果表明,CGNPs的平均药物包封率和载药量分别为64%和10±2.1%(w/w)。当样品在较低pH值下测试时,累积释放值略有向更高值的偏移。此外,体外细胞毒性测试表明,在不同浓度药物存在下48小时后,生长细胞数量显著减少。结果还表明,在低浓度(0.57µM)下,释放的药物可基于疏水和氢键相互作用通过静态机制与DNA结合。