School of Pharmacy, Harbin University of Commerce, 138, Tong Da Street, Harbin 150076, China.
Department of Pharmaceutics, Daqing Campus, Harbin Medical University, 1 Xin Yang Road, Daqing 163319, China.
Int J Biol Macromol. 2020 Apr 15;149:108-115. doi: 10.1016/j.ijbiomac.2020.01.222. Epub 2020 Jan 24.
Zedoary turmeric oil (ZTO) has a strong antitumor activity. However, its volatility, insolubility, low bioavailability, and difficulty of medication owing to oily liquid limit its clinical applications. Solid lipid nanoparticles can provide hydrophobic environment to dissolve hydrophobic drug and solidify the oily active composition to decrease the volatility and facilitate the medication. Chitosan has been widely used in pharmaceutics in recent years and coating with chitosan further enhances the internalization of particles by cells due to charge attract. Here, Chitosan (CS)-coated solid lipid nanoparticles (SLN) loaded with ZTO was prepared and characterized using dynamic laser scanner (DLS) and transmission electron microscope (TEM). The uptake and distribution of drug were evaluated in vitro and in vivo. The average sizes of ZTO-SLN and CS-ZTO-SLN were 134.3 ± 3.42 nm and 210.7 ± 4.59 nm, respectively. CS coating inverted the surface charge of particles from -8.93 ± 1.92 mV to +9.12 ± 2.03 mV. The liver accumulation of CS-ZTO-SLN was higher than ZTO-SLN (chitosan-uncoated particles) by analysis of tissue homogenate using HPLC, and the bioavailability of ZTO was also obviously improved. The results suggested that SLN coated with CS improved the features of ZTO formulation and efficiently deliver drug to the liver.
莪术油(ZTO)具有很强的抗肿瘤活性。然而,由于其挥发性、不溶性、低生物利用度以及油性液体给药困难,限制了其临床应用。固体脂质纳米粒可以为疏水性药物提供疏水环境,并将油性活性成分固化,以降低挥发性并便于给药。壳聚糖近年来在药剂学中得到了广泛应用,通过带正电荷的壳聚糖涂层进一步增强了颗粒被细胞内化的能力。本研究采用动态激光散射仪(DLS)和透射电子显微镜(TEM)制备并表征了载莪术油的壳聚糖(CS)包覆固体脂质纳米粒(SLN)。通过体外和体内实验评价了药物的摄取和分布。ZTO-SLN 和 CS-ZTO-SLN 的平均粒径分别为 134.3±3.42nm 和 210.7±4.59nm。CS 涂层使颗粒表面电荷从-8.93±1.92mV 变为+9.12±2.03mV。通过高效液相色谱法分析组织匀浆,CS-ZTO-SLN 的肝积累量高于 ZTO-SLN(未涂层颗粒),ZTO 的生物利用度也明显提高。结果表明,CS 包覆的 SLN 改善了 ZTO 制剂的特性,并能有效地将药物递送到肝脏。