Review - An update on the use of oral phospholipid excipients

Eur J Pharm Sci. 2017 Oct 15:108:1-12. doi: 10.1016/j.ejps.2017.07.008. Epub 2017 Jul 12.

Abstract

The knowledge and experiences obtained with oral phospholipid excipients is increasing continuously. Nevertheless the present number of oral products using these excipients as essential excipient is very limited. This is remarkable to note, since phospholipids play a significant role in the food uptake mechanisms of the GI tract and these mechanisms could be translated into suitable dosage forms and corresponding drug delivery strategies. In addition, phospholipid excipients are multifunctional biodegradable, non-toxic excipients, which can be used in oral dosage forms as wetting agents, emulsifier, solubilizer and matrix forming excipients. Especially natural phospholipid excipients, made from renewable sources, may be considered as environmentally friendly excipients and as a viable alternative to synthetic phospholipid and non-phospholipid analogues. This review describes 1) essential physico-chemical properties of oral phospholipid excipients 2) the fate of orally administered phospholipids with respect to absorption and metabolism in the GI tract 3) the main dosage forms used for oral administration containing phospholipids. These elements are critically assessed and areas of future research of interest for the use of oral phospholipid excipients are summarized.

Keywords: Absorption; Conversion to solids; Emulsions; Mixed micelles; Oral; Phospholipids; Solid dispersions.

Publication types

  • Review

MeSH terms

  • Administration, Oral
  • Chemistry, Pharmaceutical
  • Drug Delivery Systems / methods*
  • Emulsions / chemistry
  • Excipients / chemistry*
  • Humans
  • Micelles
  • Molecular Structure
  • Phospholipids / chemistry*
  • Solubility
  • Structure-Activity Relationship

Substances

  • Emulsions
  • Excipients
  • Micelles
  • Phospholipids