Gastrointestinal persorption and tissue distribution of differently sized colloidal gold nanoparticles

• Published in: Journal of pharmaceutical sciences Vol. 90; no. 12; pp. 1927 - 1936
• Main Authors: Hillyer, Julián F., Albrecht, Ralph M.
• Format: Journal Article
• Language: English
• Published: New York Elsevier Inc 01.12.2001; John Wiley & Sons, Inc; Wiley; American Pharmaceutical Association
• Subjects: absorption; Administration, Oral; Animals; Biological and medical sciences; colloidal gold; Digestive System - metabolism; Digestive System - ultrastructure; electron microscopy; General pharmacology; Gold Colloid - administration & dosage; Gold Colloid - pharmacokinetics; Ileum - metabolism; Ileum - ultrastructure; Intestinal Absorption; Intestinal Mucosa - metabolism; Intestinal Mucosa - ultrastructure; Medical sciences; Mice; Mice, Inbred BALB C; Microspheres; nanoparticle; Nanotechnology; neutron activation; Particle Size; persorption; Pharmaceutical technology. Pharmaceutical industry; Pharmacokinetics. Pharmacogenetics. Drug-receptor interactions; Pharmacology. Drug treatments; Tissue Distribution; neutron activation; electron microscopy; nanoparticle; colloidal gold; absorption; persorption; Neutron activation analysis; Particle size; Pharmaceutical technology; Digestive system; Nanoparticle; Persorption; Rodentia; Gut; Oral administration; Drug carrier; Vertebrata; Mammalia; Absorption; Mouse; Animal; Distribution; Dosage form
• ISSN: 0022-3549; 1520-6017
• DOI: 10.1002/jps.1143

The gastrointestinal uptake of micro‐ and nanoparticles has been the subject of recent efforts to develop effective carriers that enhance the oral uptake of drugs and vaccines. Here, we used correlative instrumental neutron activation analysis and electron microscopy to quantitatively and qualitatively study the gastrointestinal uptake and subsequent tissue/organ distribution of 4, 10, 28, and 58 nm diameter metallic colloidal gold particles following oral administration to mice. In our quantitative studies we found that colloidal gold uptake is dependent on particle size: smaller particles cross the gastrointestinal tract more readily. Electron microscopic studies showed that particle uptake occurred in the small intestine by persorption through single, degrading enterocytes in the process of being extruded from a villus. To our knowledge this is the first report, at the ultrastructural level, of gastrointestinal uptake of particulates by persorption through holes created by extruding enterocytes. © 2001 Wiley‐Liss, Inc. and the American Pharmaceutical Association J Pharm Sci 90:1927–1936, 2001