Hoshikawa Akihiro, Nagira Mizuki, Tane Masafumi, Fukushige Kaori, Tagami Tatsuaki, Ozeki Tetsuya
Drug Delivery and Nano Pharmaceutics, Graduate School of Pharmaceutical Sciences, Nagoya City University.
Biol Pharm Bull. 2018;41(6):908-914. doi: 10.1248/bpb.b18-00010.
Gold nanoparticles (GNPs) have promising properties such as photothermal effects and could be useful for imaging and as multifunctional nanocarriers for various drugs. In this study, we synthesized polyethyleneglycol (PEG)-grafted GNPs and conjugated them with cyclodextrin (CD) to incorporate curcumin. Curcumin has anticancer effects but its therapeutic application is limited due to poor water solubility. Three types of CDs (α-, β-, and γ-CDs) were conjugated with PEGylated GNPs and the curcumin-containing CD/PEG-conjugated GNPs (cur-CD-GNPs) were characterized. Transmission electron microscopy and dynamic light scattering results showed that these cur-CD-GNPs have a small gold nanocore (approximately 5 nm) and the average size of the three cur-CD-GNPs was approximately 25-35 nm. Curcumin was efficiently incorporated into the β-CD solution and the loading efficiency of curcumin in β-CD-GNPs was the highest of the three types of CD-GNPs prepared. The cytotoxic effect of cur-CD-GNPs was investigated using a human lung cancer cell line. All cur-CD-GNPs exhibited cytotoxic effects comparable to that of curcumin solution and CD-GNPs without curcumin were not cytotoxic. These results suggest that cur-CD-GNPs may be a useful multifunctional nanomedicine, although in vivo investigations are required.
金纳米颗粒(GNPs)具有诸如光热效应等有前景的特性,可用于成像以及作为各种药物的多功能纳米载体。在本研究中,我们合成了聚乙二醇(PEG)接枝的GNPs,并将其与环糊精(CD)共轭以包载姜黄素。姜黄素具有抗癌作用,但其治疗应用因水溶性差而受到限制。三种类型的CD(α-、β-和γ-CD)与聚乙二醇化的GNPs共轭,并对含姜黄素的CD/PEG共轭GNPs(cur-CD-GNPs)进行了表征。透射电子显微镜和动态光散射结果表明,这些cur-CD-GNPs具有小的金纳米核(约5nm),三种cur-CD-GNPs的平均尺寸约为25-35nm。姜黄素被有效地包载到β-CD溶液中,姜黄素在β-CD-GNPs中的负载效率是所制备的三种类型CD-GNPs中最高的。使用人肺癌细胞系研究了cur-CD-GNPs的细胞毒性作用。所有cur-CD-GNPs均表现出与姜黄素溶液相当的细胞毒性作用,而不含姜黄素的CD-GNPs没有细胞毒性。这些结果表明,cur-CD-GNPs可能是一种有用的多功能纳米药物,尽管还需要进行体内研究。