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Critical Reviews™ in Therapeutic Drug Carrier Systems
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ISSN Druckformat: 0743-4863
ISSN Online: 2162-660X

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Critical Reviews™ in Therapeutic Drug Carrier Systems

DOI: 10.1615/CritRevTherDrugCarrierSyst.v12.i4.30
pages 339-371

Targeting of Peptide and Protein Drugs to Specific Sites in the Oral Route

Jane P. F. Bai
College of Pharmacy, University of Minnesota, Minneapolis, MN 55455
Li-Ling Chang
College of Pharmacy, University of Minnesota, Minneapolis, MN 55455
Jian-Hwa Guo
3M Pharmaceuticals, 3M Center 270-4S-02, St. Paul, MN 55144

ABSTRAKT

Although the distal small intestine has less lumenal and apical proteolytic activities, it has high activities of some apical peptidases. Colonic proteolytic activities are substantial, but their nature is less understood. The small intestine has di- and tripeptide transporter, facilitating absorption, and P-glycoprotein, an efflux pump suggested to limit absorption of small peptides. Several peptide and nonpeptide drugs have higher absorption in the ileum; however, enhancement on their absorption by enhancers varies from site to site. Specific delivery systems can target drugs to the distal intestine utilizing distinct regional pHs and specific microbial enzymes, but the key is how to achieve a reliable release.


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