Department of Chemical and Biological Engineering, Korea National University of Transportation, Chungbuk 380-702, Republic of Korea.
Carbohydr Polym. 2012 Nov 6;90(4):1461-8. doi: 10.1016/j.carbpol.2012.07.016. Epub 2012 Jul 16.
This study presents an approach to deliver non invasive, near-IR imaging agent using oral delivery system. Low molecular weight heparin (LMWH)-deoxycholic acid (DOCA)/(LHD) nanoparticles formed by a self-assembly method was prepared to evaluate their physicochemical properties and oral absorption in vitro and in vivo. Near-IR QDs were prepared and loaded into LHD nanoparticles for imaging of the gastro-intestinal (GI) tract absorption. Q-LHD nanoparticles were almost spherical in shape with diameters of 194-217 nm. The size and fluorescent intensity of the Q-LHD nanoparticles were stable in 10% FBS solution and retained their fluorescent even after 5 days of incubation. Cell viability of Q-LHD nanoparticles maintained in the range of 80-95% for 24h incubation. No damage was found in tissues or organs during animal experiments. The in vivo oral absorption of Q-LHD was observed in SKH1 mice for 3h under different doses. From the results, we confirmed that Q-LHD was absorbed mostly into the ileum of small intestine containing intestinal bile acid transporter as observed in TEM and molecular imaging system. Our designed nanoparticles could be administered orally for bio-imaging and studying the bio-distribution of drug.
本研究提出了一种通过口服给药系统递送非侵入性近红外成像剂的方法。通过自组装方法制备了低分子量肝素（LMWH）-脱氧胆酸（DOCA）/（LHD）纳米粒子，以评估其理化性质以及在体外和体内的口服吸收。制备了近红外 QD 并将其装载到 LHD 纳米粒子中，以对胃肠道（GI）吸收进行成像。Q-LHD 纳米粒子呈近球形，直径为 194-217nm。在 10％FBS 溶液中，Q-LHD 纳米粒子的尺寸和荧光强度稳定，即使孵育 5 天后仍保持荧光。Q-LHD 纳米粒子的细胞活力在 24h 孵育期间保持在 80-95％的范围内。在动物实验过程中，未发现组织或器官受损。在不同剂量下，在 SKH1 小鼠中观察到 Q-LHD 在 3h 内的体内口服吸收。结果表明，Q-LHD 主要被吸收到含有肠胆酸转运体的小肠回肠中，这在 TEM 和分子成像系统中得到了观察。我们设计的纳米粒子可以口服给药用于生物成像和研究药物的生物分布。
