Imaging of the GI tract by QDs loaded heparin-deoxycholic acid (DOCA) nanoparticles

Carbohydr Polym. 2012 Nov 6;90(4):1461-8. doi: 10.1016/j.carbpol.2012.07.016. Epub 2012 Jul 16.

Abstract

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.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Administration, Oral
  • Animals
  • Anticoagulants / administration & dosage
  • Anticoagulants / chemistry
  • Anticoagulants / pharmacokinetics*
  • Caco-2 Cells
  • Cell Survival / drug effects
  • Deoxycholic Acid / administration & dosage
  • Deoxycholic Acid / chemistry
  • Deoxycholic Acid / pharmacokinetics*
  • Diagnostic Imaging*
  • Gastrointestinal Tract / drug effects
  • Heparin / administration & dosage
  • Heparin / chemistry
  • Heparin / pharmacokinetics*
  • Humans
  • Ileum / drug effects
  • Intestinal Absorption
  • Intestines / drug effects
  • Mice
  • Mice, Hairless
  • Nanoparticles / administration & dosage*
  • Nanoparticles / chemistry
  • Quantum Dots*
  • Tissue Distribution

Substances

  • Anticoagulants
  • Deoxycholic Acid
  • Heparin