Circulating Lipoproteins: A Trojan Horse Guiding Squalenoylated Drugs to LDL-Accumulating Cancer Cells.
Mol Ther
; 25(7): 1596-1605, 2017 07 05.
Article
em En
| MEDLINE
| ID: mdl-28606375
ABSTRACT
Selective delivery of anticancer drugs to rapidly growing cancer cells can be achieved by taking advantage of their high receptor-mediated uptake of low-density lipoproteins (LDLs). Indeed, we have recently discovered that nanoparticles made of the squalene derivative of the anticancer agent gemcitabine (SQGem) strongly interacted with the LDLs in the human blood. In the present study, we showed both in vitro and in vivo that such interaction led to the preferential accumulation of SQGem in cancer cells (MDA-MB-231) with high LDL receptor expression. As a result, an improved pharmacological activity has been observed in MDA-MB-231 tumor-bearing mice, an experimental model with a low sensitivity to gemcitabine. Accordingly, we proved that the use of squalene moieties not only induced the gemcitabine insertion into lipoproteins, but that it could also be exploited to indirectly target cancer cells in vivo.
Palavras-chave
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Esqualeno
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Neoplasias da Mama
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Receptores de LDL
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Adenocarcinoma
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Regulação Neoplásica da Expressão Gênica
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Nanopartículas
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Lipoproteínas LDL
Limite:
Animals
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Female
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Humans
Idioma:
En
Ano de publicação:
2017
Tipo de documento:
Article