Department of Applied Chemistry, Faculty of Chemistry, Razi University, Kermanshah, Iran.
Department of Medical Biotechnology, Faculty of Medicine, Kermanshah University of Medical Sciences, Kermanshah 6714415185, Iran.
Curr Pharm Biotechnol. 2021;22(5):622-635. doi: 10.2174/1389201021999200727153513.
Enhancement of anti-tumor activity of the chemotherapeutic agent CUR by redoxsensitive nanoparticle to get a deeper insight into cancer therapy.
Tumor targetability and stimulus are widely used to study the delivery of drugs for cancer diagnosis and treatment because poor cellular uptake and inadequate intracellular drug release lead to inefficient delivery of anticancer agents to tumor tissue.
Studies distinguishing between tumor and normal tissues or redox-sensitive systems using glutathione (GSH) as a significant signal.
In this study, we designed Chitosan-Lipoic acid Nanoparticles (CS-LANPs) to improve drug delivery for breast cancer treatment by efficient delivery of Curcumin (CUR). The properties of blank CS-LANPs were studied in detail. The size and the Polydispersity Index (PDI) of the CS-LANPs were optimized.
The results indicate the mean size and PDI of the blank CS-LANPs were around 249 nm and 0.125, respectively. However, the Drug Loading (DL) and Encapsulation Efficiency (EE) of the CSLANPs were estimated to be about 18.22% and 99.80%, respectively. Compared to non-reductive conditions, the size of reduction-sensitive CS-LANPs increased significantly under reductive conditions. Therefore, the drug release of CS-LANPs in the presence of glutathione was much faster than that of non-GSH conditions .Moreover, the antitumor effect of CS-LANPs on MCF-7 cells was determined in vitro by MTT assay, cell cytotoxicity, Caspase-3 Assay, detection of mitochondrial membrane potential and quantification of apoptosis incidence.
CS-LANPs showed a remarkably increased accumulation in tumor cells and had a better tumor inhibitory activity in vitro. CS-LANPs could successfully deliver drugs to cancer cells and revealed better efficiency than free CUR.
通过氧化还原敏感纳米粒子增强化疗药物 CUR 的抗肿瘤活性，深入了解癌症治疗。
肿瘤靶向性和刺激广泛用于研究用于癌症诊断和治疗的药物传递，因为细胞摄取不良和细胞内药物释放不足导致抗癌剂向肿瘤组织的传递效率低下。
使用谷胱甘肽 (GSH) 作为重要信号区分肿瘤和正常组织或氧化还原敏感系统的研究。
在这项研究中，我们设计了壳聚糖-硫辛酸纳米粒子 (CS-LANPs)，通过高效递送姜黄素 (CUR) 来改善乳腺癌治疗的药物传递。详细研究了空白 CS-LANPs 的性质。优化了 CS-LANPs 的粒径和多分散指数 (PDI)。
结果表明，空白 CS-LANPs 的平均粒径和 PDI 分别约为 249nm 和 0.125。然而，CS-LANPs 的载药量 (DL) 和包封效率 (EE) 估计分别约为 18.22%和 99.80%。与非还原条件相比，还原敏感 CS-LANPs 的粒径在还原条件下显著增加。因此，CS-LANPs 在谷胱甘肽存在下的药物释放速度比非 GSH 条件下快得多。此外，通过 MTT 测定、细胞毒性测定、Caspase-3 测定、线粒体膜电位检测和凋亡发生率定量，在体外测定了 CS-LANPs 对 MCF-7 细胞的抗肿瘤作用。
CS-LANPs 显示出在肿瘤细胞中明显增加的积累，并在体外具有更好的肿瘤抑制活性。CS-LANPs 可以成功地将药物递送到癌细胞中，并且比游离 CUR 具有更高的效率。
