Mucoadhesive Ionic Liquid Gel Patches for Oral Delivery,ACS Biomaterials Science & Engineering

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Mucoadhesive Ionic Liquid Gel Patches for Oral Delivery
ACS Biomaterials Science & Engineering ( IF 5.4 ) Pub Date : 2020-08-17 , DOI: 10.1021/acsbiomaterials.0c01024
Kevin Peng _{1,

2} , Yujie Shi ₁ , Anthony LaBarbiera ₁ , Samir Mitragotri _{1,

2}

Affiliation

Oral delivery of biologic drugs is a highly desired yet challenging goal because of the many barriers posed by the GI tract. Ionic liquids (ILs) and deep eutectic solvents (DESs) such as choline and geranate (CAGE) have demonstrated the potential to improve intestinal absorption of insulin and poorly soluble drugs. As with other delivery agents, localization of the ILs in the intestine can enhance the delivery potential by increasing local concentrations while maintaining low off-target concentrations, thus improving the therapeutic window of the ILs. Here, we describe a method of encapsulating CAGE into a gel using PVA, forming a mucoadhesive ionogel patch (CAGE-patch) designed to adhere to the intestine. CAGE-patches formed via repeated freeze–thaw cycles demonstrated mucoadhesive strength, swelling, and controlled release of both CAGE and insulin. In vitro transport studies revealed a more than 30% increase in insulin transport when compared to controls across Caco-2 and HT29-MTX-E12 coculture layers. This design provides a novel approach to localize ionic liquids and therapeutics in the GI tract for enhanced oral delivery.

中文翻译：

用于口服给药的粘膜粘附离子液体凝胶贴剂

由于胃肠道造成的许多障碍，生物药物的口服递送是一个非常理想但具有挑战性的目标。离子液体 (ILs) 和低共熔溶剂 (DESs)，如胆碱和天竺葵酸盐 (CAGE)，已证明具有改善胰岛素和难溶性药物的肠道吸收的潜力。与其他递送剂一样，IL 在肠道中的定位可以通过增加局部浓度同时保持低脱靶浓度来增强递送潜力，从而改善 IL 的治疗窗口。在这里，我们描述了一种使用 PVA 将 CAGE 封装到凝胶中的方法，形成粘膜粘附离子凝胶贴片（CAGE 贴片），旨在粘附在肠道上。通过反复冻融循环形成的 CAGE 斑块显示出粘膜粘附强度、肿胀、CAGE 和胰岛素的控制释放。体外转运研究显示，与跨 Caco-2 和 HT29-MTX-E12 共培养层的对照相比，胰岛素转运增加了 30% 以上。这种设计提供了一种将离子液体和治疗剂定位在胃肠道中以增强口服给药的新方法。

更新日期：2020-08-17

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