Challenges for the oral delivery of macromolecules

Nat Rev Drug Discov. 2003 Apr;2(4):289-95. doi: 10.1038/nrd1067.


The rapid integration of new technologies by the pharmaceutical industry has resulted in numerous breakthroughs in the discovery, development and manufacturing of pharmaceutical products. In particular, the commercial-scale production of high-purity recombinant proteins has resulted in important additions to treatment options for many large therapeutic areas. In addition to proteins, other macromolecules, such as the animal-derived mucopolysaccharide heparins, have also seen dramatic growth as injectable pharmaceutical products. To date, macromolecules have been limited as therapeutics by the fact that they cannot be orally delivered. This article will address the current status and future possibilities of oral macromolecular drug delivery.

Publication types

  • Review

MeSH terms

  • Administration, Oral
  • Animals
  • Biological Availability
  • Drug Delivery Systems / trends*
  • Forecasting
  • Heparin / administration & dosage*
  • Heparin / pharmacokinetics
  • Heparin / therapeutic use
  • Humans
  • Macromolecular Substances*
  • Recombinant Proteins


  • Macromolecular Substances
  • Recombinant Proteins
  • Heparin