Ahmad Mohammad, Sahabjada -, Akhtar Juber, Hussain Arshad, Badaruddeen -, Arshad Md, Mishra Anuradha
Herbal Bioactive Research Laboratory, Faculty of Pharmacy, Integral University, Lucknow, India.
Molecular Endocrinology Laboratory, Department of Zoology, University of Lucknow, Lucknow, India.
EXCLI J. 2017 May 31;16:810-823. doi: 10.17179/excli2016-668. eCollection 2017.
Biological effects of rutin bioactive are limited due to its poor oral bioavailability and its degradation in aqueous environments. For the purpose of bioenhancement, different nanoemulsion systems of rutin were developed by aqueous titration method using water as dispersion media. The nanoemulsion systems were characterized for surface morphology, droplet size, polydispersity index, zeta potential, release profile and the formulations were optimized. The anticancer potential of optimized nanoemulsion was evaluated by cells viability (MTT) assay, nuclear condensation, and ROS activity using human prostate cancer (PC3) cell line. On the basis of cell viability data the inhibitory concentration (IC) value for optimized nanoemulsion formulation on PC3 cancer cells was found to be 11.8 μM. Fluorescent microscopic analysis and intracellular ROS generation demonstrated significant ROS induction that might lead to triggering the apoptosis pathway. In conclusion, developed nanoemulsion displayed significant efficacy against prostate carcinoma cells.
芦丁生物活性成分的生物学效应有限,这是由于其口服生物利用度差以及在水性环境中易降解。为了实现生物增强,采用水相滴定法,以水作为分散介质,开发了不同的芦丁纳米乳剂系统。对纳米乳剂系统的表面形态、液滴大小、多分散指数、zeta电位、释放曲线进行了表征,并对配方进行了优化。通过细胞活力(MTT)测定、核浓缩和使用人前列腺癌(PC3)细胞系的ROS活性评估了优化纳米乳剂的抗癌潜力。根据细胞活力数据,发现优化纳米乳剂配方对PC3癌细胞的抑制浓度(IC)值为11.8 μM。荧光显微镜分析和细胞内ROS生成表明,显著的ROS诱导可能导致触发凋亡途径。总之,所开发的纳米乳剂对前列腺癌细胞显示出显著的疗效。