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Adv Drug Deliv Rev. 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.

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Purdue University, Departments of Biomedical Engineering & Pharmaceutics, West Lafayette, IN, USA.


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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