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Intestinal permeation enhancers: Lessons learned from studies using an organ culture model.
Biochimica et Biophysica Acta (BBA) - Biomembranes ( IF 2.8 ) Pub Date : 2020-09-16 , DOI: 10.1016/j.bbamem.2020.183474
E Michael Danielsen 1
Affiliation  

Permeation enhancers (PEs) are compounds aimed to increase intestinal uptake of oral drugs with poor bioavailability. This mini-review focuses on results recently obtained with PEs using an intestinal organ culture model. The model predicts which paracellular/transcellular pathways across the epithelium are susceptible to different classes of PEs (mainly surfactants and cell penetrating peptides). PEs: 1) generate a transmembrane transcellular pathway, 2) block apical endocytosis (first step in apical-to-basolateral transcytosis), and 3) perturb normal cell membrane integrity. The results argue that surfactants and cell penetrating peptides are not suitable for use in formulations aimed to exploit transcytosis in oral drug delivery.



中文翻译:

肠渗透促进剂:使用器官培养模型从研究中学到的经验教训。

渗透促进剂(PEs)是旨在提高生物利用度较差的口服药物肠道吸收的化合物。这份小型回顾重点在于最近使用肠器官培养模型通过PE获得的结果。该模型预测穿过上皮的哪些细胞旁/跨细胞途径易受不同种类的PE(主要是表面活性剂和细胞穿透肽)的影响。PE:1)产生跨膜跨细胞通路,2)阻止顶尖内吞作用(顶尖到基底外侧转胞作用的第一步),以及3)扰乱正常细胞膜的完整性。结果认为表面活性剂和细胞穿透肽不适合用于旨在利用口服药物传递中的胞吞作用的制剂中。

更新日期:2020-09-20
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