Oral delivery of peptides and proteins using lipid-based drug delivery systems.
BACKGROUND
In order to successfully develop lipid-based drug delivery systems (DDS) for oral administration of peptides and proteins, it is important to gain an understanding of the colloid structures formed by these DDS, the mode of peptide and protein incorporation as well as the mechanism by which intestinal absorption of peptides and proteins is promoted.


METHODS
The present paper reviews the literature on lipid-based DDS, employed for oral delivery of peptides and proteins and highlights the mechanisms by which the different lipid-based carriers are expected to overcome the two most important barriers (extensive enzymatic degradation and poor transmucosal permeability). This paper also gives a clear-cut idea about advantages and drawbacks of using different lipidic colloidal carriers ((micro)emulsions, solid lipid core particles and liposomes) for oral delivery of peptides and proteins.


CONCLUSIONS
Lipid-based DDS are safe and suitable for oral delivery of peptides and proteins. Significant progress has been made in this area with several technologies on clinical trials. However, a better understanding of the mechanism of action in vivo is needed in order to improve the design and development of lipid-based DDS with the desired bioavailability and therapeutic profile.
University of Copenhagen, Faculty of Health and Medical Sciences, Department of Pharmacy, 2100 Copenhagen Ø, Denmark. amu@farma.ku.dk
Ping
P
Li
Hanne Mørck
HM
Nielsen
Anette
A
Müllertz
D000284:Administration, Oral; D000818:Animals; D001682:Biological Availability; D004337:Drug Carriers; D016503:Drug Delivery Systems; D004655:Emulsions; D006801:Humans; D007408:Intestinal Absorption; D008055:Lipids; D008081:Liposomes; D010455:Peptides / Q000008:administration & dosage* / Q000737:chemistry / Q000378:metabolism; D010539:Permeability; D011506:Proteins / Q000008:administration & dosage* / Q000737:chemistry / Q000378:metabolism
D004337:Drug Carriers; D004655:Emulsions; D008055:Lipids; D008081:Liposomes; D010455:Peptides; D011506:Proteins