Department of Chemistry, School of Physical and Mathematical Sciences, University of Kerala, Kariavattom, Thiruvananthapuram 695 581, Kerala, India.
Department of Chemistry, School of Physical and Mathematical Sciences, University of Kerala, Kariavattom, Thiruvananthapuram 695 581, Kerala, India.
Int J Biol Macromol. 2016 Jul;88:222-35. doi: 10.1016/j.ijbiomac.2016.03.040. Epub 2016 Mar 21.
Curcumin (Cur), a poly phenolic yellow colored compound present in Indian spice turmeric, has a wide variety of biological properties. Bioavailability of Cur is limited by its low water solubility, rapid metabolism and low stability. In the present study, we mainly focus on synthesis and characterization of dextran based nano-sized drug carrier (GHDx) for the delivery of Cur. A liver targeting moiety is incorporated in GHDx so as to improve the therapeutic efficiency and decrease adverse effects of conventional cancer therapy. The effect of different parameters on grafting variables was studied. GHDx was characterised by FTIR, (1)H NMR XRD, TG/DTG, TEM, SEM, AFM, DLS and zeta potential analyses. Adsorption experiments were carried out for drug loading. Swelling of GHDx was studied as a function of pH and temperature. Three step release of Cur from GHDx was confirmed by analyzing in vitro release data in simulated intracellular pH using different kinetic models. In vitro cytotoxicity analysis on L929 and Hep G2 cells shows that GHDx is safe carrier while Cur loaded GHDx exhibits high toxicity with slow drug release towards hepatic cells. The results show that the GHDx can be customized as a stimuli sensitive potential carrier for the delivery of drugs.
姜黄素（Cur）是一种存在于印度香料姜黄中的多酚黄色化合物，具有广泛的生物学特性。Cur 的生物利用度受到其低水溶性、快速代谢和低稳定性的限制。在本研究中，我们主要专注于合成和表征基于葡聚糖的纳米药物载体（GHDx），用于输送 Cur。在 GHDx 中掺入肝靶向部分，以提高治疗效率并降低传统癌症治疗的不良反应。研究了不同参数对接枝变量的影响。通过傅里叶变换红外光谱（FTIR）、（1）H 核磁共振（NMR）、X 射线衍射（XRD）、热重分析/差示扫描量热法（TG/DTG）、透射电子显微镜（TEM）、扫描电子显微镜（SEM）、原子力显微镜（AFM）、动态光散射（DLS）和 Zeta 电位分析对 GHDx 进行了表征。进行了吸附实验以进行药物负载。研究了 GHDx 的溶胀作为 pH 和温度函数的情况。通过使用不同的动力学模型分析模拟细胞内 pH 下的体外释放数据，证实了 Cur 从 GHDx 的三步骤释放。在 L929 和 Hep G2 细胞上进行的体外细胞毒性分析表明，GHDx 是一种安全的载体，而负载 Cur 的 GHDx 对肝细胞表现出高毒性和缓慢的药物释放。结果表明，GHDx 可以定制为一种刺激响应性潜在药物载体，用于药物输送。
