Roy Partha, Das Suvadra, Auddy Runa Ghosh, Mukherjee Arup
Division of Pharmaceutical and Fine Chemicals Technology, Department of Chemical Technology, University of Calcutta, Kolkata, India ; Faculty of Technology (Pharmaceutical), Universiti Malaysia, Pahang, Malaysia.
Division of Pharmaceutical and Fine Chemicals Technology, Department of Chemical Technology, University of Calcutta, Kolkata, India.
Int J Nanomedicine. 2014 Oct 9;9:4723-35. doi: 10.2147/IJN.S65262. eCollection 2014.
Andrographolide (AG) is one of the most potent labdane diterpenoid-type free radical scavengers available from plant sources. The compound is the principal bioactive component in Andrographis paniculata leaf extracts, and is responsible for anti-inflammatory, anticancer, and immunomodulatory activity. The application of AG in therapeutics, however, is severely constrained, due to its low aqueous solubility, short biological half-life, and poor cellular permeability. Engineered nanoparticles in biodegradable polymer systems were therefore conceived as one solution to aid in further drug-like applications of AG. In this study, a cationic modified poly(lactic-co-glycolic) acid nanosystem was applied for evaluation against experimental mouse hepatotoxic conditions. Biopolymeric nanoparticles of hydrodynamic size of 229.7 ± 17.17 nm and ζ-potential +34.4 ± 1.87 mV facilitated marked restoration in liver functions and oxidative stress markers. Superior dissolution for bioactive AG, hepatic residence, and favorable cytokine regulation in the liver tissues are some of the factors responsible for the newer nanosystem-assisted rapid recovery.
穿心莲内酯（AG）是从植物来源获得的最有效的半日花烷二萜类自由基清除剂之一。该化合物是穿心莲叶提取物中的主要生物活性成分，具有抗炎、抗癌和免疫调节活性。然而，由于AG的低水溶性、短生物半衰期和较差的细胞通透性，其在治疗中的应用受到严重限制。因此，可生物降解聚合物系统中的工程化纳米颗粒被认为是有助于AG进一步类似药物应用的一种解决方案。在本研究中，一种阳离子改性聚乳酸-乙醇酸纳米系统被用于评估实验性小鼠肝毒性情况。流体动力学尺寸为229.7±17.17 nm且ζ电位为+34.4±1.87 mV的生物聚合物纳米颗粒有助于肝功能和氧化应激标志物的显著恢复。生物活性AG的优异溶解性、肝脏滞留以及肝脏组织中有利的细胞因子调节是导致新型纳米系统辅助快速恢复的一些因素。
