Studies on PEGylated Gold Nanoparticles Loaded with 5-Hydroxydecanoate for Chemo-Photothermal Therapy of Human Lung AdenocarcinomasIn Vitro

Abstract

Gold nanoparticles (Au NPs) have promising applications in the¯elds of drug delivery and photothermal therapy. 5-hydroxydecanoate (5-HD) is a kind of highly selective mitochondrial ATP sensitive potassium (mitoKATP) channel blocker. In this research,¯rstly, 5-HD was studied whether it could induce human lung adenocarcinomas (A549) cells apoptosis; secondly, PEGylated gold nanoparticles loaded with 5-HD (Au NPs-PEG-5-HD) were prepared to develop a new chemotherapy and photothermal therapy in one system under the irradiation of green light-emitting diode (LED). Subsequently, in vitro cytotoxicity test was analyzed by cell counting kit-8 (CCK-8), the change of mitochondrial membrane potential (Á m) was determined by immuno°uorescence microscopy with R-123°uorescence, and cell apoptosis and necrosis rate were detected by°ow cytometry. The results of CCK8 revealed that the inhibition rates of A549 cells were all greatly increased when cells were treated with free 5-HD, free 5-HD þLED irradiation, Au NPs-PEG-5-HD and Au NPs-PEG-5-HDþLED irradiation, and Au NPs-PEG-5-HD had enhanced cell-killing e®ect compared with 5-HD, furthermore, the Au NPs-PEG-5-HD and LED irradiation played a very great synergy e®ect. The immuno°uorescence microscopy data ‡ Corresponding author. 1550101-1NANO: Brief Reports and Reviews Vol. 10, No. 7 (2015) also exhibited a reduction of Á m correspondingly. Flow cytometric analysis showed that the apoptosis rate of cells that were incubated with free 5-HD, 5-HDþLED irradiation, Au NPs-PEG-5-HD or Au NPs-PEG-5-HDþLED irradiation signi¯cantly increased to about 9.2%, 10.7%, 18.3% or 12.4% and the percentage of necrosis cells increased to around 8.8%, 9.7%, 48.0% or 69.8%, respectively. In a word, all the results indicated that the 5-HD had shown the ability to induce A549 cells apoptosis as a chemotherapy agent, and its ability would be improved when 5-HD is loaded on PEGylated Au NPs, as well as Au NPs-PEG-5-HD exhibited signi¯-cantly enhanced photothermal e®ects for treatment of lung adenocarcinomas.