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Titolo:
STRUCTURAL REQUIREMENTS FOR INTESTINAL-ABSORPTION OF PEPTIDE DRUGS
Autore:
PAULETTI GM; GANGWAR S; KNIPP GT; NERURKAR MM; OKUMU FW; TAMURA K; SIAHAAN TJ; BORCHARDT RT;
Indirizzi:
UNIV KANSAS,DEPT PHARMACEUT CHEM,2095 CONSTANT AVE LAWRENCE KS 66047 UNIV KANSAS,DEPT PHARMACEUT CHEM LAWRENCE KS 66047
Titolo Testata:
Journal of controlled release
fascicolo: 1-2, volume: 41, anno: 1996,
pagine: 3 - 17
SICI:
0168-3659(1996)41:1-2<3:SRFIOP>2.0.ZU;2-F
Fonte:
ISI
Lingua:
ENG
Soggetto:
BRUSH-BORDER MEMBRANE; RAT SMALL-INTESTINE; THYROTROPIN-RELEASING-HORMONE; BETA-LACTAM ANTIBIOTICS; ANGIOTENSIN-CONVERTING ENZYME; EPITHELIAL-CELL MONOLAYERS; HAMSTER JEJUNUM INVITRO; RABBIT SMALL-INTESTINE; CACO-2 CELLS; TIGHT JUNCTIONS;
Keywords:
PEPTIDE DELIVERY; INTESTINAL BARRIER FUNCTIONS; PEPTIDE MODIFICATIONS; PRODRUGS; PEPTIDASE INHIBITORS;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Science Citation Index Expanded
Citazioni:
143
Recensione:
Indirizzi per estratti:
Citazione:
G.M. Pauletti et al., "STRUCTURAL REQUIREMENTS FOR INTESTINAL-ABSORPTION OF PEPTIDE DRUGS", Journal of controlled release, 41(1-2), 1996, pp. 3-17

Abstract

The clinical development of orally active peptide drugs has been restricted by their unfavorable physicochemical characteristics, which limit their membrane permeation, and their lack of stability against enzymatic degradation. Successful oral delivery of peptides will depend, therefore, on strategies designed to alter the physicochemical properties of these potential drugs, without changing their biological activity, in order to circumvent the barrier properties of the intestinal epithelial cells. This manuscript will focus on the physical and metabolic barrier functions of the intestinal mucosa, the structural features of peptides which influence their passive diffusion and carrier-mediated transport, including efflux mechanisms, and various approaches usedto prevent enzymatic degradation of the peptides and increase their permeability across the intestinal mucosa.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 25/11/20 alle ore 15:12:38