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Review
. 2013 Jun 15;65(6):822-32.
doi: 10.1016/j.addr.2012.10.007. Epub 2012 Nov 2.

Nanoparticles for oral delivery: targeted nanoparticles with peptidic ligands for oral protein delivery

Yeonhee Yun  1 , Yong Woo Cho, Kinam Park
Affiliations
Review

Nanoparticles for oral delivery: targeted nanoparticles with peptidic ligands for oral protein delivery

Yeonhee Yun et al. Adv Drug Deliv Rev. .

Abstract

As the field of biotechnology has advanced, oral protein delivery has also made significant progress. Oral delivery is the most common method of drug administration with high levels of patient acceptance. Despite the preference of oral delivery, administration of therapeutic proteins has been extremely difficult. Increasing the bioavailability of oral protein drugs to the therapeutically acceptable level is still a challenging goal. Poor membrane permeability, high molecular weight, and enzymatic degradation of protein drugs have remained unsolved issues. Among diverse strategies, nanotechnology has provided a glimpse of hope in oral delivery of protein drugs. Nanoparticles have advantages, such as small size, high surface area, and modification using functional groups for high capacity or selectivity. Nanoparticles with peptidic ligands are especially worthy of notice because they can be used for specific targeting in the gastrointestinal (GI) tract. This article reviews the transport mechanism of the GI tract, barriers to protein absorption, current status and limitations of nanotechnology for oral protein delivery system.

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Figures

Figure 1
Figure 1
Schematic representation of the transport mechanisms: (a) receptor-mediated transport; (b) carrier-mediated transport; (c) paracellular transport; (d) transcellular transport; and (e) M cell mediated transport (i.e., phagocytosis by M cells).
Figure 2
Figure 2
The effect of ACGDRGDCFCG-murine tumor necrosis factor-conjugate (RGD-mTNF) on tumor growth and body weight of animal-bearing RMA tumors. 5 mice/group were treated intraperitoneal at day 10 with melphalan alone or in combination with RGD-mTNF or CNGRCG-mTNF conjugate (NGR-mTNF) at the indicated doses (A). Loss of animal weight at day 1 and day 4 after treatment (B) [87].
Figure 3
Figure 3
Schematic illustration of targeted nanoparticles with peptidic ligands.
Figure 4
Figure 4
In vivo localization of CKS9 compared with CSK9 in rat small intestinal tissues. Chemically synthesized CKS9 or CSK9 was injected into closed ileal loops and their tissue specific localization was monitored under fluorescence-microscopy; (a and b) in vivo localization of CSK9 peptides in Peyer’s patches and Non- Peyer’s patches. (c and d) in vivo localization of CKS9 peptides in Peyer’s patches and Non- Peyer’s patches. Green and red fluorescent signals in each panel indicate the location of the peptides and mucus layer in rat small intestinal tissues (closed ileal loops), respectively. Scale bars indicate 50 mm in Peyer’s patches and 20 mm in Non- Peyer’s patches, respectively [112].
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