Skip to main page content
U.S. flag

An official website of the United States government

Dot gov

The .gov means it’s official.
Federal government websites often end in .gov or .mil. Before sharing sensitive information, make sure you’re on a federal government site.

Https

The site is secure.
The https:// ensures that you are connecting to the official website and that any information you provide is encrypted and transmitted securely.

Access keys NCBI Homepage MyNCBI Homepage Main Content Main Navigation
. 2013 Nov;4(11):1443-67.
doi: 10.4155/tde.13.104.

Basics and recent advances in peptide and protein drug delivery

Benjamin J Bruno  1 , Geoffrey D Miller, Carol S Lim
Affiliations

Basics and recent advances in peptide and protein drug delivery

Benjamin J Bruno et al. Ther Deliv. 2013 Nov.

Abstract

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.

PubMed Disclaimer

Figures

Figure 1
Figure 1
Common routes of administration for systemic delivery of peptides and proteins.
Figure 2
Figure 2. Intestinal barriers to peptide delivery
The epithelial intestinal barrier is made up of a single layer of columnar epithelial cells. The apical side of the barrier contains the mucosal layer. Drugs may penetrate the epithelial barrier either through the transcellular route (across the cell) or the paracellular route (between tight junctions). See text for other term explanations.
Figure 3
Figure 3. Solid lipid nanoparticle
Solid lipid nanoparticles have a solid lipid core and is coated with surfactant. Targeting moieties may be added to decorate the surface of the solid lipid nanoparticle. Cargo for solid lipid nanoparticle are illustrated as peptides or proteins, but may also include siRNA or small-molecule drugs.
Figure 4
Figure 4. Gastrointestinal mucoadhesive patch system
The system contains four layered films in an enteric capsule. Layer one is the backing layer, layer two is the middle or drug layer, layer three is the adhesive layer, and layer four is the surface layer.
See this image and copyright information in PMC

References

    1. Craik DJ, Fairlie DP, Liras S, Price D. The future of peptide-based drugs. Chem. Biol. Drug Des. 2013;81(1):136–147. - PubMed
    1. Department of health and human services . US FDA. Background document for meeting of advisory committee for reproductive health drugs and drug safety and risk management advisory committee. Vol. 113. MD, USA: 2013.
    1. Novartis . Novartis Annual Report. Basel, Switzerland: 2013.
    1. Zacks Investment Research; Novartis AG . Brokerage Research Digest. IL, USA: 2013.
    1. Mitchell M. The medicines company reports full year and fourth quarter 2011 financial results. NJ, USA: 2012.