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Peptide-Based Delivery of Oligonucleotides Across Blood–Brain Barrier Model |
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| Authors: | Artita Srimanee Jakob Regberg Mattias Hallbrink Kaido Kurrikoff Kadi-Liis Veiman Opa Vajragupta Ülo Langel |
| Institution: | 1. Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Mahidol University, 447 Sri-Ayudhya Rd., Bangkok, 10400, Thailand 2. Department of Neurochemistry, The Arrhenius Laboratories for Natural Sciences, Stockholm University, Svante Arrhenius v?g 21A, 106 91, Stockholm, Sweden 3. Institute of Technology, University of Tartu, Nooruse 1, 50411, Tartu, Estonia 4. Excellent Center for Innovation in Drug Design and Discovery, Faculty of Pharmacy, Mahidol University, 447 Sri-Ayudhya Rd., Bangkok, 10400, Thailand |
| Abstract: | 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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