Peptide-Based Delivery of Oligonucleotides Across Blood–Brain Barrier Model

被引：0

作者：

Artita Srimanee

Jakob Regberg

Mattias Hallbrink

Kaido Kurrikoff

Kadi-Liis Veiman

Opa Vajragupta

Ülo Langel

机构：

[1] Mahidol University,Department of Pharmaceutical Chemistry, Faculty of Pharmacy

[2] Stockholm University,Department of Neurochemistry, The Arrhenius Laboratories for Natural Sciences

[3] University of Tartu,Institute of Technology

[4] Mahidol University,Excellent Center for Innovation in Drug Design and Discovery, Faculty of Pharmacy

来源：

International Journal of Peptide Research and Therapeutics | 2014年 / 20卷

关键词：

Blood–brain barrier model; Cell-penetrating peptide; Glioma cells; bEnd.3; Plasmid transfection; Gene-based therapy;

D O I：

暂无

中图分类号：

学科分类号：

摘要：

Delivery of pharmaceutical agents across a blood–brain barrier (BBB) is a challenge for brain cancer therapy. In this study, an in vitro BBB model was utilized to study the delivery of oligonucleotides across brain endothelial cells targeting to glioma cells in a Transwell™ setup. A series of novel peptides were synthesized by covalent conjugation of cell-penetrating peptides with targeting peptides for delivery of gene-based therapeutics. These peptides were screened for passage across the Transwell™ and we found the most efficient peptide PepFect32 from originating PepFect 14 coupled with the targeting peptide angiopep-2. PepFect32/pDNA nanocomplexes exhibited high transcytosis across the BBB in vitro model and the highest transfection efficiency to glioma cells. In conclusion, PepFect32 revealed the most efficient peptide-based vector for pDNA delivery across in vitro BBB model.

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页码：169 / 178

页数：9

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