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Chitosan mediated solid lipid nanoparticles for enhanced liver delivery of zedoary turmeric oil in vivo
International Journal of Biological Macromolecules ( IF 7.7 ) Pub Date : 2020-01-24 , DOI: 10.1016/j.ijbiomac.2020.01.222
Bo Yang , Jiaqi Jiang , Lei Jiang , Peiyu Zheng , Fuling Wang , Yang Zhou , Zhong Chen , Minghui Li , Mingming Lian , Shukun Tang , Xiaoying Liu , Haisheng Peng , Qun Wang

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.



中文翻译:

壳聚糖介导的固体脂质纳米颗粒可增强zedoary姜黄油在体内的肝脏输送

Zedoary姜黄油(ZTO)具有很强的抗肿瘤活性。然而,其挥发性,不溶性,低生物利用度以及由于油性液体而引起的用药困难限制了其临床应用。固体脂质纳米颗粒可提供疏水性环境以溶解疏水性药物并固化油性活性组合物,以降低挥发性并促进药物治疗。近年来,壳聚糖已被广泛用于药物领域,并且由于电荷吸引,壳聚糖包衣进一步增强了颗粒被细胞内化的能力。在这里,制备了负载有ZTO的壳聚糖(CS)涂层的固体脂质纳米颗粒(SLN),并使用动态激光扫描仪(DLS)和透射电子显微镜(TEM)对其进行了表征。摄取和药物的分布进行评价体外体内。ZTO-SLN和CS-ZTO-SLN的平均尺寸分​​别为134.3±3.42 nm和210.7±4.59 nm。CS涂层将颗粒的表面电荷从-8.93±1.92 mV反转为+9.12±2.03 mV。通过HPLC分析组织匀浆,CS-ZTO-SLN的肝蓄积高于ZTO-SLN(壳聚糖未包被的颗粒),ZTO的生物利用度也明显提高。结果表明,涂​​有CS的SLN改善了ZTO配方的功能,并有效地将药物递送至肝脏。

更新日期:2020-01-24
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