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Characterization of Particulate Drug Delivery Systems for Oral Delivery of Peptide and Protein Drugs

[ Vol. 21 , Issue. 19 ]


Philip Carsten Christophersen, Mathias Fano, Lasse Saaby, Mingshi Yang, Hanne Mørck Nielsen and Huiling Mu   Pages 2611 - 2628 ( 18 )


Oral drug delivery is a preferred route because of good patient compliance. However, most peptide/ protein drugs are delivered via parenteral routes because of the absorption barriers in the gastrointestinal (GI) tract such as enzymatic degradation by proteases and low permeability acrossthe biological membranes. To overcome these barriers, different formulation strategies for oral delivery of biomacromolecules have been proposed, including lipid based formulations and polymer-based particulate drug delivery systems (DDS). The aim of this review is to summarize the existing knowledge about oral delivery of peptide/protein drugs and to provide an overview of formulationand characterization strategies. For a better understanding of the challenges in oral delivery of peptide/protein drugs, the composition of GI fluids and the digestion processes of different kinds of excipients in the GI tract are summarized. Additionally, the paper provides an overview of recent studies on characterization of solid drug carriers for peptide/protein drugs, drug distribution in particles, drug release and stability in simulated GI fluids, as well as the absorption of peptide/protein drugs in cell-based models. The use of biorelevant media when applicable can increase the knowledge about the quality of DDS for oral protein delivery. Hopefully, the knowledge provided in this review will aid the establishment of improved biorelevant models capable of forecasting the performance of particulate DDS for oral peptide/protein delivery.


Oral drug delivery, peptide/protein drugs, particulate delivery systems, solid lipid particles, drug release mechanism, stability, lipolysis, in vitro methods.


Department of Pharmacy, Universitetsparken 2, 2100 Copenhagen;

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