Exploring Intestinal Surface Receptors in Oral Nanoinsulin Delivery,Pharmacological Reviews

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Exploring Intestinal Surface Receptors in Oral Nanoinsulin Delivery
Pharmacological Reviews ( IF 19.3 ) Pub Date : 2022-10-01 , DOI: 10.1124/pharmrev.122.000631
Carlynne Choy ₁ , Lee Yong Lim ₁ , Lai Wah Chan ₁ , Zhixiang Cui ₁ , Shirui Mao ₁ , Tin Wui Wong ₂

Affiliation

Subcutaneous and inhaled insulins are associated with needle phobia, lipohypertrophy, lipodystrophy, and cough in diabetes treatment. Oral nanoinsulin has been developed, reaping the physiologic benefits of peroral administration. This review profiles intestinal receptors exploitable in targeted delivery of oral nanoinsulin. Intestinal receptor targeting improves oral insulin bioavailability and sustains blood glucose–lowering response. Nonetheless, these studies are conducted in small animal models with no optimization of insulin dose, targeting ligand type and content, and physicochemical and molecular biologic characteristics of nanoparticles against the in vivo/clinical diabetes responses as a function of the intestinal receptor population characteristics with diabetes progression. The interactive effects between nanoinsulin and antidiabetic drugs on intestinal receptors, including their up-/downregulation, are uncertain. Sweet taste receptors upregulate SGLT-1, and both have an undefined role as new intestinal targets of nanoinsulin. Receptor targeting of oral nanoinsulin represents a viable approach that is relatively green, requiring an in-depth development of the relationship between receptors and their pathophysiological profiles with physicochemical attributes of the oral nanoinsulin.

中文翻译：

探索口服纳米胰岛素递送中的肠表面受体

皮下和吸入胰岛素与糖尿病治疗中的针头恐惧症、脂肪肥大、脂肪营养不良和咳嗽有关。口服纳米胰岛素已经开发出来，获得了口服给药的生理益处。本综述介绍了可用于靶向递送口服纳米胰岛素的肠道受体。靶向肠道受体可提高口服胰岛素的生物利用度并维持降血糖反应。尽管如此，这些研究是在小动物模型中进行的，没有优化胰岛素剂量、靶向配体类型和含量，以及纳米粒子对体内/临床糖尿病反应的物理化学和分子生物学特性作为糖尿病肠道受体群特征的函数进展。纳米胰岛素和抗糖尿病药物对肠道受体的相互作用，包括它们的上调/下调，尚不确定。甜味受体上调 SGLT-1，两者作为纳米胰岛素的新肠道靶标都具有不确定的作用。口服纳米胰岛素的受体靶向代表了一种相对绿色的可行方法，需要深入研究受体及其病理生理学特征与口服纳米胰岛素的理化特性之间的关系。

更新日期：2022-09-30

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