Pharmaceutical Research

, Volume 14, Issue 3, pp 259–266

The Oral Absorption of Micro- and Nanoparticulates: Neither Exceptional Nor Unusual

Authors

  • Alexander T. Florence
    • Centre for Drug Delivery Research, School of PharmacyUniversity of London
Article

DOI: 10.1023/A:1012029517394

Cite this article as:
Florence, A.T. Pharm Res (1997) 14: 259. doi:10.1023/A:1012029517394

Abstract

This mini-review covers some of the historical and recent arguments over the experimental evidence on the uptake by and translocation from the intestinal mucosa of microparticulates after oral administration. It is concluded that there is now no dispute over the fact that this is a normal occurrence. Particulate uptake does take place, not only via the M-cells in the Peyer's patches and the isolated follicles of the gut-associated lymphoid tissue, but also via the normal intestinal enterocytes. Factors affecting uptake include particle size, surface charge and hydrophobicity and the presence or absence of surface ligands. The covalent attachment of lectin or invasin molecules to the surface of carrier particles leads to greater systemic uptake. Whether or not the route can be utilized for the routine administration of therapeutic agents which are not normally absorbed from the gut is not yet proven. Many studies show that 2−3% of the ingested dose of submicron particles can be absorbed. The increasing diversity of carrier systems, which includes dendrimers and liposomes, needs to be exploited fully. More also must be learned about the inter- and intra-subject variability of lymphoid tissue so that appropriate selectivity can be achieved through the design of specific carriers.

microparticlesPeyer's patchesGALTparticle absorptionoral deliverylymphatics
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Copyright information

© Plenum Publishing Corporation 1997