Lipid-based nanocarriers for the oral administration of biopharmaceutics

Nanomedicine (Lond). 2016 Nov;11(22):3009-3032. doi: 10.2217/nnm-2016-0265. Epub 2016 Oct 26.

Abstract

Biopharmaceutics have been recognized as the drugs of choice for the treatment of several diseases, mainly due to their high selectivity and potent action. Nonetheless, their oral administration is a rather challenging problem, since their bioavailability is significantly hindered by various physiological barriers along the GI tract, including their acid-induced hydrolysis in the stomach, their enzymatic degradation throughout the GI tract and their poor mucosa permeability. Lipid-based nanocarriers represent a viable means for enhancing the oral bioavailability of biomolecules while diminishing toxicity-related issues. The present review describes the main physiological barriers limiting the oral bioavailability of macromolecules and highlights recent advances in the field of lipid-based carriers as well as the respective lipid intestinal absorption mechanisms.

Keywords: SEDDS; biopharmaceutics; emulsions; lipid-based drug delivery systems; liposomes; oral delivery; solid lipid particles.

MeSH terms

  • Administration, Oral
  • Biopharmaceutics*
  • Drug Carriers / administration & dosage
  • Drug Carriers / chemistry*
  • Gastrointestinal Tract / drug effects
  • Gastrointestinal Tract / physiology
  • Humans
  • Intestinal Absorption / drug effects
  • Lipids / administration & dosage
  • Lipids / chemistry*
  • Nanoparticles / administration & dosage
  • Nanoparticles / chemistry*

Substances

  • Drug Carriers
  • Lipids