Benefit of a Short Chain Peptide as a Targeting Ligand of Nanocarriers for a Brain-Driven Purpose
Treatment of glioma remains a critical challenge worldwide, since the therapeutic effect is greatly hindered by poor transportation across the blood brain barrier (BBB) and low penetration into tumor cells. In this study, a peptide-conjugated nano-delivery system was explored for the purpose of glio...
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| Published in | Pharmaceutics Vol. 13; no. 8; p. 1249 |
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| Main Authors | , |
| Format | Journal Article |
| Language | English |
| Published |
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12.08.2021
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| Abstract | Treatment of glioma remains a critical challenge worldwide, since the therapeutic effect is greatly hindered by poor transportation across the blood brain barrier (BBB) and low penetration into tumor cells. In this study, a peptide-conjugated nano-delivery system was explored for the purpose of glioma therapy. A peptide-decorated copolymer was used to prepare nanoparticles (NPs) by a solvent evaporation method. The particle size was in the range of 160.9 ± 3.3–173.5 ± 3.6 nm with monodistribution, and the zeta potentials ranged from −18.6 ± 1.2 to +7.9 ± 0.6 mV showing an increasing trend with R9-peptide. An in vitro cocultured BBB model illustrated the internalization of peptide-conjugated NPs in bEnd.3 cells followed by uptake by U87-MG cells indicating both BBB-crossing and glioma-penetrating abilities. IVIS (In Vivo Imaging System) images revealed that T7-conjugated NPs specifically accumulated in the brain more than peptide-free NPs and had less biodistribution in nontarget tissues than T7/R9 dual-peptide conjugated NPs. The benefit of T7-peptide as a targeting ligand for NPs across the BBB with accumulation in the brain was elucidated. |
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| AbstractList | Treatment of glioma remains a critical challenge worldwide, since the therapeutic effect is greatly hindered by poor transportation across the blood brain barrier (BBB) and low penetration into tumor cells. In this study, a peptide-conjugated nano-delivery system was explored for the purpose of glioma therapy. A peptide-decorated copolymer was used to prepare nanoparticles (NPs) by a solvent evaporation method. The particle size was in the range of 160.9 ± 3.3–173.5 ± 3.6 nm with monodistribution, and the zeta potentials ranged from −18.6 ± 1.2 to +7.9 ± 0.6 mV showing an increasing trend with R9-peptide. An in vitro cocultured BBB model illustrated the internalization of peptide-conjugated NPs in bEnd.3 cells followed by uptake by U87-MG cells indicating both BBB-crossing and glioma-penetrating abilities. IVIS (In Vivo Imaging System) images revealed that T7-conjugated NPs specifically accumulated in the brain more than peptide-free NPs and had less biodistribution in nontarget tissues than T7/R9 dual-peptide conjugated NPs. The benefit of T7-peptide as a targeting ligand for NPs across the BBB with accumulation in the brain was elucidated. Treatment of glioma remains a critical challenge worldwide, since the therapeutic effect is greatly hindered by poor transportation across the blood brain barrier (BBB) and low penetration into tumor cells. In this study, a peptide-conjugated nano-delivery system was explored for the purpose of glioma therapy. A peptide-decorated copolymer was used to prepare nanoparticles (NPs) by a solvent evaporation method. The particle size was in the range of 160.9 ± 3.3-173.5 ± 3.6 nm with monodistribution, and the zeta potentials ranged from -18.6 ± 1.2 to +7.9 ± 0.6 mV showing an increasing trend with R9-peptide. An in vitro cocultured BBB model illustrated the internalization of peptide-conjugated NPs in bEnd.3 cells followed by uptake by U87-MG cells indicating both BBB-crossing and glioma-penetrating abilities. IVIS (In Vivo Imaging System) images revealed that T7-conjugated NPs specifically accumulated in the brain more than peptide-free NPs and had less biodistribution in nontarget tissues than T7/R9 dual-peptide conjugated NPs. The benefit of T7-peptide as a targeting ligand for NPs across the BBB with accumulation in the brain was elucidated.Treatment of glioma remains a critical challenge worldwide, since the therapeutic effect is greatly hindered by poor transportation across the blood brain barrier (BBB) and low penetration into tumor cells. In this study, a peptide-conjugated nano-delivery system was explored for the purpose of glioma therapy. A peptide-decorated copolymer was used to prepare nanoparticles (NPs) by a solvent evaporation method. The particle size was in the range of 160.9 ± 3.3-173.5 ± 3.6 nm with monodistribution, and the zeta potentials ranged from -18.6 ± 1.2 to +7.9 ± 0.6 mV showing an increasing trend with R9-peptide. An in vitro cocultured BBB model illustrated the internalization of peptide-conjugated NPs in bEnd.3 cells followed by uptake by U87-MG cells indicating both BBB-crossing and glioma-penetrating abilities. IVIS (In Vivo Imaging System) images revealed that T7-conjugated NPs specifically accumulated in the brain more than peptide-free NPs and had less biodistribution in nontarget tissues than T7/R9 dual-peptide conjugated NPs. The benefit of T7-peptide as a targeting ligand for NPs across the BBB with accumulation in the brain was elucidated. |
| Author | Lo, Yu-Chen Lin, Wen-Jen |
| AuthorAffiliation | 1 School of Pharmacy, College of Medicine, National Taiwan University, Taipei 10050, Taiwan; elisa50626@gmail.com 2 Drug Research Center, College of Medicine, National Taiwan University, Taipei 10050, Taiwan |
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| Title | Benefit of a Short Chain Peptide as a Targeting Ligand of Nanocarriers for a Brain-Driven Purpose |
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