Models to predict intestinal absorption of therapeutic peptides and proteins
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Models to predict intestinal absorption of therapeutic peptides and proteins. / Antunes, Filipa; Andrade, Fernanda; Ferreira, Domingos; Nielsen, Hanne Mørck; Sarmento, Bruno.
In: Current Drug Metabolism, Vol. 14, No. 1, 01.2013, p. 4-20.Research output: Contribution to journal › Journal article › Research › peer-review
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TY - JOUR
T1 - Models to predict intestinal absorption of therapeutic peptides and proteins
AU - Antunes, Filipa
AU - Andrade, Fernanda
AU - Ferreira, Domingos
AU - Nielsen, Hanne Mørck
AU - Sarmento, Bruno
PY - 2013/1
Y1 - 2013/1
N2 - Prediction of human intestinal absorption is a major goal in the design, optimization, and selection of drugs intended for oral delivery, in particular proteins, which possess intrinsic poor transport across intestinal epithelium. There are various techniques currently employed to evaluate the extension of protein absorption in the different phases of drug discovery and development. Screening protocols to evaluate protein absorption include a range of preclinical methodologies like in silico, in vitro, in situ, ex vivo and in vivo. It is the careful and critical use of these techniques that can help to identify drug candidates, which most probably will be well absorbed from the human intestinal tract. It is well recognized that the human intestinal permeability cannot be accurately predicted based on a single preclinical method. However, the present social and scientific concerns about the animal well care as well as the pharmaceutical industries need for rapid, cheap and reliable models predicting bioavailability give reasons for using methods providing an appropriate correlation between results of in vivo and in vitro drug absorption. The aim of this review is to describe and compare in silico, in vitro, in situ, ex vivo and in vivo methods used to predict human intestinal absorption, giving a special attention to the intestinal absorption of therapeutic peptides and proteins.
AB - Prediction of human intestinal absorption is a major goal in the design, optimization, and selection of drugs intended for oral delivery, in particular proteins, which possess intrinsic poor transport across intestinal epithelium. There are various techniques currently employed to evaluate the extension of protein absorption in the different phases of drug discovery and development. Screening protocols to evaluate protein absorption include a range of preclinical methodologies like in silico, in vitro, in situ, ex vivo and in vivo. It is the careful and critical use of these techniques that can help to identify drug candidates, which most probably will be well absorbed from the human intestinal tract. It is well recognized that the human intestinal permeability cannot be accurately predicted based on a single preclinical method. However, the present social and scientific concerns about the animal well care as well as the pharmaceutical industries need for rapid, cheap and reliable models predicting bioavailability give reasons for using methods providing an appropriate correlation between results of in vivo and in vitro drug absorption. The aim of this review is to describe and compare in silico, in vitro, in situ, ex vivo and in vivo methods used to predict human intestinal absorption, giving a special attention to the intestinal absorption of therapeutic peptides and proteins.
KW - Drug screening
KW - In vitro/in vivo correlation
KW - Intestinal absorption
KW - Permeability prediction
KW - Therapeutic proteins
UR - http://www.scopus.com/inward/record.url?scp=84871348189&partnerID=8YFLogxK
U2 - 10.2174/138920013804545160
DO - 10.2174/138920013804545160
M3 - Journal article
C2 - 21933113
AN - SCOPUS:84871348189
VL - 14
SP - 4
EP - 20
JO - Current Drug Metabolism
JF - Current Drug Metabolism
SN - 1389-2002
IS - 1
ER -
ID: 239817550