A review of advanced oral drug delivery technologies facilitating the protection and absorption of protein and peptide molecules

The oral delivery of proteins and peptides is a dynamic research field despite the numerous challenges limiting their effective delivery. Successful oral delivery of proteins and peptides requires the accomplishment of three key tasks: protection of the macromolecules from degradation in the gastroi...

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Veröffentlicht in:Biotechnology advances 2014-11, Vol.32 (7), p.1269-1282
Hauptverfasser: Choonara, Bibi F., Choonara, Yahya E., Kumar, Pradeep, Bijukumar, Divya, du Toit, Lisa C., Pillay, Viness
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container_end_page 1282
container_issue 7
container_start_page 1269
container_title Biotechnology advances
container_volume 32
creator Choonara, Bibi F.
Choonara, Yahya E.
Kumar, Pradeep
Bijukumar, Divya
du Toit, Lisa C.
Pillay, Viness
description The oral delivery of proteins and peptides is a dynamic research field despite the numerous challenges limiting their effective delivery. Successful oral delivery of proteins and peptides requires the accomplishment of three key tasks: protection of the macromolecules from degradation in the gastrointestinal tract (GIT), permeation through the intestinal barrier and absorption of molecules into the systemic circulation. Currently, no clinically useful oral formulations have been developed but several attempts have been made to overcome the challenges of low oral bioavailability resulting from poor absorption, poor permeation and enzymatic degradation of the proteins and peptides in the GIT. Present strategies attempt to provide structural protection of the proteins and peptides and improved absorption through the use of enzyme inhibitors, absorption enhancers, novel polymeric delivery systems and chemical modification. However, each of these technologies has their limitations despite showing positive results. This review attempts to discuss the physical and chemical barriers of the GIT with particular emphasis on the current approaches employed to overcome these barriers, including the evaluation of other non-parenteral routes of protein and peptide delivery. In addition, this review assimilates oral formulation strategies under development and within the clinical trial stage in relation to their benefits and drawbacks with regard to facilitating optimal protection and absorption of proteins and peptides, as well as pertinent future challenges and opportunities governing oral drug delivery. •Discusses current approaches to overcome GIT absorption barriers for macromolecules•Elaborates on advanced oral macromolecular technologies for clinical application•Critically evaluates oral macromolecule systems developed and in clinical trials•Provides a critical analysis of the inherent pharmacokinetic advancements
doi_str_mv 10.1016/j.biotechadv.2014.07.006
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subjects Administration, Oral
Advanced oral biotechnology
Animals
Barriers
Bioavailability
Biological and medical sciences
Biological Availability
Biotechnology
Degradation
Drug Carriers
Drug Delivery Systems
Fundamental and applied biological sciences. Psychology
Gastrointestinal barrier
Humans
Inhibitors
Intestinal Absorption
Mice
Models, Biological
Oral drug delivery
Penetration
Peptides
Peptides - administration & dosage
Peptides - pharmacokinetics
Permeation
Proteins
Proteins - administration & dosage
Proteins - pharmacokinetics
Therapeutic proteins and peptides
title A review of advanced oral drug delivery technologies facilitating the protection and absorption of protein and peptide molecules
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