Uptake and transport of furanodiene in Caco-2 cell monolayers： a comparison study between furanodiene and furanodiene loaded PLGA nanoparticles  

作　　者：LI Gang LIN Dong-Hai XIE Xin-Xin QIN Li-Fang WANG Jun-Teng LIU Ke 

机构地区：[1]Life School of Yantai University, Yantai 264005, China [2]Pharmacy School of Yantai University, Yantai 264005, China

出　　处：《中国天然药物》2013年第1期49-55,共7页

基　　金：This project was supported by the National Natural Science Foundation of China （No. 30973949）, the Natural Science Founda- tion of Shandong Province, China （No. ZR2~012） and the Young and Middle-Aged Scientists Research Awards Foundation of Shangdong Prov- ince. China （No. BS2012YY039）.

摘　　要：目的 Furanodiene (FDE ) 与高 lipophilicity 和差的稳定性拥有多样的药理学活动。这研究准备了 FDE 由自发的乳剂溶剂散开方法装载了 PLGA nanoparticles (FDE-PLGA-NPs ) 和 PEGylated PLGA nanoparticles (FDE-PEG-PLGA-NPs ) 改进 FDE 的稳定性和 bioavailability。方法 FDE-PLGA-NPs 和 FDE-PEG-PLGA-NPs 为尺寸被描绘并且缩放分发，表面形态学，希腊语的第六个字母潜力和陷阱效率。在生理的液体(PBS 和人工的胃肠的液体) 的 FDE， FDE-PLGA-NPs 和 FDE-PEG-PLGA-NPs 的稳定性被评估。在 vitro，细胞的举起和运输研究用 Caco-2 房间单层被执行。结果 FDE-PLGA-NPs 和 FDE-PEG-PLGA-NPs 的尺寸从 110-140 nm ，分别地，陷阱效率是 87.3% 和 89.2% ，稳定性与 FDE 相比显著地被提高。FDE-PLGA-NPs 和 FDE-PEG-PLGA-NPs 能被 Caco-2 房间自由地收起并且搬运单层到对面。当 FDE 几乎没到达到受体方面时，它能被收起进 Caco-2 房间单层。这些结果显示了那 FDE-PLGA-NPs 的结论，特别 FDE-PEG-PLGA-NPs，能提高 FDE 的稳定性和 hydrophilicity 并且越过 Caco-2 房间单层增加 FDE 的浸透。AIM： Furanodiene （FDE） possesses diverse pharmacological activities with high lipophilicity and poor stability. This study prepared FDE loaded PLGA nanoparticles （FDE-PLGA-NPs） and PEGylated PLGA nanoparticles （FDE-PEG-PLGA-NPs） by the spontaneous emulsion solvent diffusion method to improve the stability and bioavailability of FDE. METHODS： FDE-PLGA-NPs and FDE-PEG-PLGA-NPs were characterized for size and size distribution, surface morphology, zeta-potential and entrapment effi- ciency. The stability of FDE, FDE-PLGA-NPs and FDE-PEG-PLGA-NPs in physiological fluids （PBS and artificial gastrointestinal fluids） was evaluated. In vitro cellular uptake and transport studies were performed using Caco-2 cell monolayers. RESULTS： The size of FDE-PLGA-NPs and FDE-PEG-PLGA-NPs ranged from 110-140 rim, the entrapment efficiencies were 87.3% and 89.2%, respec- tively, and the stabilities were enhanced significantly compared with FDE. FDE-PLGA-NPs and FDE-PEG-PLGA-NPs could be taken up by Caco-2 cells freely and transported across the monolayers. While FDE hardly reached to the receptor side, it could be taken up into Caco-2 cell monolayers. CONCLUSIONS： These results indicated that FDE-PLGA-NPs, especially FDE-PEG-PLGA-NPs, could enhance the stability and hydrophilicity of FDE and increase the permeation of FDE across Caco-2 cell monolayers.

关 键 词：呋喃二烯 Caco-2单层细胞 摄取 转运 

分 类 号：R969.1[医药卫生—药理学]