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Ther Deliv. 2013 Nov;4(11):1443-67. doi: 10.4155/tde.13.104.

Basics and recent advances in peptide and protein drug delivery.

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Department of Pharmaceutics & Pharmaceutical Chemistry, College of Pharmacy, University of Utah. 30 South 2000 East, Room 301, Salt Lake City, UT 84112, USA.


While the peptide and protein therapeutic market has developed significantly in the past decades, delivery has limited their use. Although oral delivery is preferred, most are currently delivered intravenously or subcutaneously due to degradation and limited absorption in the gastrointestinal tract. Therefore, absorption enhancers, enzyme inhibitors, carrier systems and stability enhancers are being studied to facilitate oral peptide delivery. Additionally, transdermal peptide delivery avoids the issues of the gastrointestinal tract, but also faces absorption limitations. Due to proteases, opsonization and agglutination, free peptides are not systemically stable without modifications. This review discusses oral and transdermal peptide drug delivery, focusing on barriers and solutions to absorption and stability issues. Methods to increase systemic stability and site-specific delivery are also discussed.

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