Enzyme-Triggered Intestine-Specific Targeting Adhesive Platform for Universal Oral Drug Delivery

用于通用口服药物输送的酶触发肠道特异性靶向粘附平台

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作者:Ying Li, Jung Seung Lee, Ameya R Kirtane, Mengyuan Li, Charles William Coffey 3rd, Kaitlyn Hess, Aaron Lopes, Joy Collins, Siddartha Tamang, Keiko Ishida, Alison Hayward, Jacob Wainer, Adam J Wentworth, Giovanni Traverso

Abstract

Patient adherence to chronic therapies can be suboptimal, leading to poor therapeutic outcomes. Dosage forms that enable reduction in dosing frequency stand to improve patient adherence. Variation in gastrointestinal transit time, inter-individual differences in gastrointestinal physiology and differences in physicochemical properties of drugs represent challenges to the development of such systems. To this end, a small intestine-targeted drug delivery system is developed, where prolonged gastrointestinal retention and sustained release are achieved through tissue adhesion of drug pills mediated by an essential intestinal enzyme catalase. Here proof-of-concept pharmacokinetics is demonstrated in the swine model for two drugs, hydrophilic amoxicillin and hydrophobic levodopa. It is anticipated that this system can be applicable for many drugs with a diverse of physicochemical characteristics.

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