A 7-ketocholesterol containing-nanoemulsion (LDE/7KC) inhibits growth of melanoma tumor in mice and increases survival rate / Nanoemulsão contendo 7-cetocolesterol (LDE/7KC) promove inibição do crescimento de melanoma em camundongos e aumento de sobrevida

AUTOR(ES)
DATA DE PUBLICAÇÃO

2007

RESUMO

7-ketocholesterol (7KC) is an oxysterol known to inhibit cell proliferation and to be cytotoxic. A nanoemulsion containing-7KC (LDE/7KC) was shown to have antiproliferative effects on RPMI 8226 myeloma cell line and melanoma (B16F10), in vitro. This particle is taken up mainly by LDL receptors. Here we have evaluated the plasma kinetic, biodistribution, anti-tumoral action and hematologic toxicity of LDE/7KC in melanoma bearing mice. The nanoemulsion accumulated in the liver and tumor, tissues with a high expression of LDL receptors. LDE/7KC promoted a tumor size reduction over fifty percent. An increased necrosis area and a decreased amount of blood vessels were found. An increased survival rate was observed. The hematolgic analyses demonstrated a lack of toxicicity. The results shows the possibility to use the LDE/7KC nanoemulsion as an agent for cancer treatment, with few collateral effects probably due to its internalization by LDL receptors.

ASSUNTO(S)

receptores ldl pharmacokinetics. cetocolesteróis melanoma experimental emulsões ldl lipoprotein emulsions ketocholesterol melanoma ldl receptor lipoproteínas do colesterol ldl farmacocinética

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