Polyelectrolyte complexes as prospective carriers for the oral delivery of protein therapeutics

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• 作者：Vassilis Bourganis^a ; Theodora Karamanidou^a ; Olga Kammona^b ; Costas Kiparissides^a ; ^b ; ^{costas.kiparissides@cperi.certh.gr}
• 关键词：Polyelectrolytes ; Polyelectrolyte complexes ; Oral delivery ; Drug delivery systems ; Colloidal nanocarriers ; Proteins ; Mucosa
• 刊名：European Journal of Pharmaceutics and Biopharmaceutics
• 出版年：2017
• 出版时间：February 2017
• 年：2017
• 卷：111
• 期：Complete
• 页码：44-60
• 全文大小：2571 K
• 卷排序：111

文摘

The oral administration of protein therapeutics is hindered by the multitude of barriers confronted by these molecules along the gastrointestinal tract (i.e., acidic environment, proteolytic degradation, mucosal barrier, etc.). Their unique properties (e.g., high molecular weight, hydrophilicity, charge, etc.) and labile structure are mainly responsible for their instability in the harsh conditions along the gastrointestinal tract (GIT) and dictate the employment of alternative routes for their administration (e.g., parenteral). The association of proteins with colloidal carriers represents an interesting approach to overcome the aforementioned issues. However, certain requirements, such as stability in the GIT, stimuli-responsiveness, protection of the encapsulated biomolecule from enzymatic degradation and permeability of the mucosa, have to be met in order to efficiently deliver the sensitive payload to the intended site of action, thus resulting in enhanced bioavailability. The formation of colloidal polyelectrolyte complexes (PECs) seems to be a promising strategy towards this direction, and the present review aims to provide an insight into PECs (e.g., preparation methods, characteristics) along with their advantages and drawbacks as drug delivery vehicles for the oral administration of protein-based therapeutics.