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Cholesterol-Peptide Hybrids to Form Liposome-Like Vesicles for Gene Delivery

In this paper, four amphiphilic cholesterol-peptide conjugates (Ch-R5H5, Ch-R3H3, Ch-R5 and Ch-R5) were designed and synthesized, and their properties in gene delivery were evaluated in vitro with an aim of developing more efficient gene delivery carriers. These amphiphilic cholesterol-peptide conju...

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Autores principales: Tang, Qiong, Cao, Bin, Wu, Haiyan, Cheng, Gang
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Public Library of Science 2013
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3559823/
https://www.ncbi.nlm.nih.gov/pubmed/23382899
http://dx.doi.org/10.1371/journal.pone.0054460
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author Tang, Qiong
Cao, Bin
Wu, Haiyan
Cheng, Gang
author_facet Tang, Qiong
Cao, Bin
Wu, Haiyan
Cheng, Gang
author_sort Tang, Qiong
collection PubMed
description In this paper, four amphiphilic cholesterol-peptide conjugates (Ch-R5H5, Ch-R3H3, Ch-R5 and Ch-R5) were designed and synthesized, and their properties in gene delivery were evaluated in vitro with an aim of developing more efficient gene delivery carriers. These amphiphilic cholesterol-peptide conjugates are composed of hydrophobic cholesterol and positively charged peptides. They were able to self-assemble into micelles at low concentrations and their critical micelle concentrations in phosphate buffered saline (pH 7.4) are ≤85 µg/mL. Amphiphilic cholesterol-peptide conjugates condensed DNA more efficiently than a hydrophilic cationic oligoarginine (R10) peptide with no hydrophobic segment. Their transfection efficiencies were at least two orders of magnitude greater than that of R10 peptide in HEK-293 cells. Moreover, the introduction of histidine residues in cholesterol-peptide conjugates led to higher gene expression efficiency compared with cholesterol-peptides without histidine (Ch-R5 and Ch-R3), and the luciferase expression level was comparable or even higher than that induced by PEI at its optimal N/P ratio. In particular, Ch-R5H5 condensed DNA into smaller nanoparticles than Ch-R3H3 at higher N/P ratios, and the minimum size of Ch-R5H5/DNA complexes was 180 nm with zeta potential of 23 mV, achieved at the N/P ratio of 30. This liposome-like vesicle may be a promising gene delivery carrier for intravenous therapy.
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spelling pubmed-35598232013-02-04 Cholesterol-Peptide Hybrids to Form Liposome-Like Vesicles for Gene Delivery Tang, Qiong Cao, Bin Wu, Haiyan Cheng, Gang PLoS One Research Article In this paper, four amphiphilic cholesterol-peptide conjugates (Ch-R5H5, Ch-R3H3, Ch-R5 and Ch-R5) were designed and synthesized, and their properties in gene delivery were evaluated in vitro with an aim of developing more efficient gene delivery carriers. These amphiphilic cholesterol-peptide conjugates are composed of hydrophobic cholesterol and positively charged peptides. They were able to self-assemble into micelles at low concentrations and their critical micelle concentrations in phosphate buffered saline (pH 7.4) are ≤85 µg/mL. Amphiphilic cholesterol-peptide conjugates condensed DNA more efficiently than a hydrophilic cationic oligoarginine (R10) peptide with no hydrophobic segment. Their transfection efficiencies were at least two orders of magnitude greater than that of R10 peptide in HEK-293 cells. Moreover, the introduction of histidine residues in cholesterol-peptide conjugates led to higher gene expression efficiency compared with cholesterol-peptides without histidine (Ch-R5 and Ch-R3), and the luciferase expression level was comparable or even higher than that induced by PEI at its optimal N/P ratio. In particular, Ch-R5H5 condensed DNA into smaller nanoparticles than Ch-R3H3 at higher N/P ratios, and the minimum size of Ch-R5H5/DNA complexes was 180 nm with zeta potential of 23 mV, achieved at the N/P ratio of 30. This liposome-like vesicle may be a promising gene delivery carrier for intravenous therapy. Public Library of Science 2013-01-30 /pmc/articles/PMC3559823/ /pubmed/23382899 http://dx.doi.org/10.1371/journal.pone.0054460 Text en © 2013 Tang et al http://creativecommons.org/licenses/by/4.0/ This is an open-access article distributed under the terms of the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original author and source are properly credited.
spellingShingle Research Article
Tang, Qiong
Cao, Bin
Wu, Haiyan
Cheng, Gang
Cholesterol-Peptide Hybrids to Form Liposome-Like Vesicles for Gene Delivery
title Cholesterol-Peptide Hybrids to Form Liposome-Like Vesicles for Gene Delivery
title_full Cholesterol-Peptide Hybrids to Form Liposome-Like Vesicles for Gene Delivery
title_fullStr Cholesterol-Peptide Hybrids to Form Liposome-Like Vesicles for Gene Delivery
title_full_unstemmed Cholesterol-Peptide Hybrids to Form Liposome-Like Vesicles for Gene Delivery
title_short Cholesterol-Peptide Hybrids to Form Liposome-Like Vesicles for Gene Delivery
title_sort cholesterol-peptide hybrids to form liposome-like vesicles for gene delivery
topic Research Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3559823/
https://www.ncbi.nlm.nih.gov/pubmed/23382899
http://dx.doi.org/10.1371/journal.pone.0054460
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