School of Nano Sciences, Central University of Gujarat, Gandhinagar 382030, Gujarat, India.
School of Life Science, Central University of Gujarat, Gandhinagar 382030, Gujarat, India.
Int J Pharm. 2020 Oct 15;588:119795. doi: 10.1016/j.ijpharm.2020.119795. Epub 2020 Aug 25.
Carvacrol (CV), a monoterpene possesses wide range of biological activities but has limited application due to low aqueous solubility and poor bioavailability. To address this issue and enhance bioavailability and efficacy of carvacrol, lecithin stabilized zein nanoparticles were investigated. Precipitation method was used for synthesis of nanoparticles and characterized using various techniques. CV entrapped under optimized parameters has size around 250 nm with -15 mV zeta potential. SEM studies showed nanoparticles with spherical morphology and size in accordance with DLS studies. FTIR, NMR and DSC were used to determine the molecular interaction between CV and lecithin stabilized zein nanoparticles. Molecular docking studies were performed to understand the interaction between protein and drug at molecular level. Our results demonstrated the presence of two active sites within zein, showing strong binding interactions with carvacrol. The encapsulation efficiency of 78% with loading efficiency of 13% was obtained as per HPLC and UV-Vis studies. Cytotoxicity assay indicated that the CV loaded nanoparticles induce cytotoxicity against colon cancer (SW480) cells further confirmed by acridine orange and ethidium bromide dual staining assay. Fluorescent tagged nanoparticles revealed significant cellular uptake of drug. Our results suggest that CV can be conveniently delivered via oral route after incorporating into lecithin stabilized zein nanoparticles and may prove effective for colon cancer treatment.
香芹酚（CV）是一种单萜类化合物，具有广泛的生物活性，但由于水溶性低和生物利用度差，其应用受到限制。为了解决这个问题，提高香芹酚的生物利用度和疗效，研究了大豆蛋白稳定的卵磷脂纳米粒。采用沉淀法合成纳米粒，并采用多种技术进行了表征。在优化参数下，CV 的包封率约为 78%，载药量为 13%，包封的 CV 粒径约为 250nm，zeta 电位为-15mV。SEM 研究表明，纳米粒具有球形形态和与 DLS 研究一致的粒径。傅里叶变换红外光谱（FTIR）、核磁共振（NMR）和差示扫描量热法（DSC）用于确定 CV 与大豆蛋白稳定的卵磷脂纳米粒之间的分子相互作用。分子对接研究用于了解蛋白质和药物在分子水平上的相互作用。我们的结果表明，大豆蛋白中存在两个活性部位，与香芹酚表现出很强的结合相互作用。根据 HPLC 和紫外-可见分光光度法的研究，包封效率为 78%，载药效率为 13%。细胞毒性试验表明，负载 CV 的纳米粒对结肠癌细胞（SW480）具有细胞毒性，吖啶橙和溴化乙锭双重染色试验进一步证实了这一点。荧光标记的纳米粒显示出药物的显著细胞摄取。我们的结果表明，CV 可以通过口服途径给药，在将其包封到大豆蛋白稳定的卵磷脂纳米粒中后，可以有效地治疗结肠癌。
