与它们的线性对应物相比,分支透丁和透马克斯显示了增强的肠道胰岛素输送效能
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Updated: May 26, 2025

An In Ovo Model for Testing Insulin-mimetic Compounds
Published on: April 23, 2018
Ragna Guldsmed Diedrichsen1, Narendra Kumar Mishra2, Freja Fredholt1
1Center for Biopharmaceuticals and Biobarriers in Drug Delivery (BioDelivery), Department of Pharmacy, Faculty of Health and Medical Sciences, University of Copenhagen, Universitetsparken 2, 2100 Copenhagen, Denmark.
像penetratin这样的分支细胞透可以显著提高它们口服药物传递的能力. 这些修改后的可以增强货物的透性,显示出口服生物制药输送的前景.
科学领域:
- 生物制药物供应提供.
- 药物透增强 药物透增强 药物透增强
- 细胞透类.
背景情况:
- 生物制药的口服输送是具有挑战性的,因为其透性较低.
- 细胞透 (CPPs) 可以增强跨越生物障碍的药物运输.
- 修改CPP,例如通过分支,可能会提高其有效性.
研究的目的:
- 通过创建二聚和三聚变体来增强透和透的增强透性特性.
- 评估分支对各种货物的横穿透的影响.
- 调查口服药物输送的分支CPPs的体内疗效.
主要方法:
- 使用Caco-2细胞培养模型来评估胰岛素,德克斯,曼尼托尔和美托普罗罗尔的穿透.
- 对比线性,二度和三度版本的穿透素和穿透素.
- 使用胰岛素作为货物进行了体内药理动力学和组织学评估.
主要成果:
- 分支显著增加了penetratin和penetramax的提高透性的特性.
- 增强的货物透度与分支的程度相关.
- 体修饰诱导了Caco-2细胞单层完整性和细胞骨架的可逆变化.
- 在体内研究证实了二次性透马克斯作为胰岛素的口服载体的潜力.
结论:
- 通过分支的基修饰有效地增强了货物透,可能是通过细胞通路.
- 分支CPPs,特别是二次性penetramax,显示出改善口服生物制药输送的巨大潜力.
- 进一步开发分支CPP可以克服口服药物管理中的重大障碍.
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