Centre for Advanced Studies in Botany, University of Madras, Chennai 600 025, Tamilnadu, India.
CHORD, CSIR-Central Leather Research Institute, Adayar, Chennai 600 020, Tamilnadu, India.
Carbohydr Polym. 2017 Mar 15;160:184-193. doi: 10.1016/j.carbpol.2016.12.049. Epub 2016 Dec 23.
The current study is to develop a natural drug carrier with seaweed derived polymers namely κ-Carrageenan (κ-Car) for drug delivery applications. κ-Car is a natural polysaccharide which derived from edible red seaweeds, they are easily available, non-toxic, cost effective, biodegradable and biocompatible nature. Curcumin (Cur) is a yellow-orange polyphenol existing in turmeric, which is predominantly used as spice and food coloring agent. The ultimate use of polymeric composites, especially those composed of natural polymers, has become a very interesting approach in recent drug delivery applications, due to their non-toxicity and biological origin. In this study the primary approach which depends on the loading of Curcumin into κ-Carrageenan was accomplished, and which (κ-Car-Cur) an active drug carrier was developed for drug delivery against selected lung cancer cells (A549). Thus, the κ-Car-Cur was synthesized by solvent evaporation method followed by freeze drying, and it was further characterized. From this study, it has been reported that the high encapsulation efficiency, good stability, and successful release of Cur from the carrier (κ-Car) was achieved. The drug release was more active at acidic pH 5.0 with the cumulative release of 78%, which is the favorable condition present in tumor microenvironments. The in vitro cellular applications studies of κ-Car-Cur demonstrated that, κ-Car-Cur composites induced higher cytotoxicity against selected cancer cells than free Cur and effectively involved to trigger cellular apoptosis in A549 cancer cells. Further, it was also possessed that inhibition of cell growth and changes in metabolic activity of cancer cells are the unique characteristic features of cellular apoptosis, through reactive oxygen species (ROS) generation. It also observed that there was a decrease in mitochondrial membrane potential (ΔψmΔψm) which leads to a cellular apoptosis during treatment with κ-Car-Cur. Hence, the study outcomes may provide the potential outline for the use of κ-Car-Cur as a promising tool to deliver drugs at intracellular level.
本研究旨在开发一种基于海藻衍生聚合物的天然药物载体，即κ-卡拉胶（κ-Car），用于药物传递应用。κ-Car 是一种天然多糖，来源于可食用的红海藻，它们易于获取、无毒、成本效益高、可生物降解且具有生物相容性。姜黄素（Cur）是存在于姜黄中的一种黄色橙色多酚，主要用作香料和食用色素。由于其无毒和生物来源，聚合物复合材料，特别是由天然聚合物组成的复合材料，在最近的药物传递应用中成为一种非常有趣的方法。在本研究中，完成了主要依赖于姜黄素负载到 κ-卡拉胶的方法，并开发了用于针对选定肺癌细胞（A549）的药物传递的活性药物载体（κ-Car-Cur）。因此，通过溶剂蒸发法随后进行冷冻干燥合成了 κ-Car-Cur，并对其进行了进一步的表征。从这项研究中，可以报道实现了高包封效率、良好的稳定性以及从载体（κ-Car）中成功释放姜黄素。在酸性 pH5.0 下，药物释放更加活跃，累积释放率为 78%，这是肿瘤微环境中存在的有利条件。κ-Car-Cur 的体外细胞应用研究表明，κ-Car-Cur 复合材料对选定的癌细胞具有更高的细胞毒性，比游离姜黄素更有效，并能有效触发 A549 癌细胞的细胞凋亡。此外，还观察到通过活性氧（ROS）的产生，抑制细胞生长和改变癌细胞的代谢活性是细胞凋亡的独特特征。还观察到在治疗期间，κ-Car-Cur 会导致线粒体膜电位（ΔψmΔψm）下降，从而导致细胞凋亡。因此，该研究结果可能为κ-Car-Cur 作为在细胞内水平递药的有前途的工具提供潜在的依据。
