Novel cationic lipids possessing protonated cyclen and imidazolium salt for gene delivery.
Eur J Pharm Biopharm
; 78(3): 326-35, 2011 Aug.
Article
em En
| MEDLINE
| ID: mdl-21439377
ABSTRACT
In this study, two novel protonated cyclen and imidazolium salt-containing cationic lipids differing only in their hydrophobic region (cholesterol or diosgenin) have been designed and synthesized for gene delivery. Cationic liposomes were easily prepared from each of these lipids individually or from the mixtures of each cationic lipid and dioleoylphosphatidyl ethanolamine (DOPE). Several studies including DLS, gel retardation assay, ethidium bromide intercalation assay, and TEM demonstrated that these amphiphilic molecules are able to bind and compact DNA into nanometer particles that could be used as non-viral gene delivery agents. Our results from in vitro transfection showed that in association with DOPE, two cationic lipids can induce effective gene transfection in HEK293 cells. Furthermore, the gene transfection efficiencies of two cationic lipids were dramatically increased in the presence of calcium ion (Ca(2+)). It is notable that the gene transfection abilities of two cationic lipids were maintained in the presence of 10% serum. Besides, different cytotoxicity was found for two lipoplexes. This study demonstrates that the title cationic lipids have large potential to be efficient non-viral gene vector.
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Terapia Genética
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Sistemas de Liberação de Medicamentos
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Compostos Heterocíclicos
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Imidazóis
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Lipídeos
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Lipossomos
Limite:
Humans
Idioma:
En
Revista:
Eur J Pharm Biopharm
Ano de publicação:
2011
Tipo de documento:
Article