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聚两性离子-聚电解质体系中的凝聚作用及其在胃肠道药物传递平台中的潜在应用。

Coacervation in polyzwitterion-polyelectrolyte systems and their potential applications for gastrointestinal drug delivery platforms.

机构信息

Department of Polymer Science and Engineering, University of Massachusetts, Amherst, MA, 01003, USA.

Rush Medical College, Rush University Medical Center, Chicago, IL, 60612, USA.

出版信息

Nat Commun. 2022 Apr 26;13(1):2250. doi: 10.1038/s41467-022-29851-y.

Abstract

Traditionally, complex coacervation is regarded as a process whereby two oppositely charged polyelectrolytes self-assemble into spherical droplets. Here, we introduce the polyzwitterionic complex, "pZC", formed by the liquid-liquid phase separation of a polyzwitterion and a polyelectrolyte, and elucidate a mechanism by which such complexes can assemble using theory and experimental evidence. This system exhibits orthogonal phase behavior-it remains intact in acidic conditions, but disassembles as the pH increases, a process governed by the acid-base equilibria of the constituent chains. We relate the observed phase behavior to physiological conditions within the gastrointestinal tract with a simulation of the gastroduodenal junction, and demonstrate using video microscopy the viability of polyzwitterionic coacervates as technologies for the pH-triggered release of cargo. Such a system is envisaged to tackle imminent problems of drug transport via the oral route and serve as a packaging solution to increase uptake efficiency.

摘要

传统上,复杂凝聚被认为是两种带相反电荷的聚电解质自组装成球形液滴的过程。在这里,我们引入了聚两性离子复合物“pZC”,它是由聚两性离子和聚电解质的液-液相分离形成的,并通过理论和实验证据阐明了这种复合物可以通过这种机制组装的机制。该系统表现出正交相行为——在酸性条件下保持完整,但随着 pH 值的增加而分解,这一过程受组成链的酸碱平衡控制。我们将观察到的相行为与胃肠道内的生理条件相关联,并通过胃十二指肠交界处的模拟来证明,使用视频显微镜证明聚两性离子凝聚物作为 pH 触发释放货物的技术的可行性。预计这样的系统将解决通过口服途径输送药物的紧迫问题,并作为一种包装解决方案来提高吸收率。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/27f3/9042848/74cd24d2c7c3/41467_2022_29851_Fig1_HTML.jpg

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