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首页> 外文期刊>Anti-cancer agents in medicinal chemistry >Targeting the Folate Receptor: Effects of Conjugating Folic Acid to DOX Loaded Polymeric Micelles
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Targeting the Folate Receptor: Effects of Conjugating Folic Acid to DOX Loaded Polymeric Micelles

机译:靶向叶酸受体:叶酸与DOX负载的聚合物胶束的共轭作用

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In this paper, we report on a potential cancer drug delivery system that utilizes the ligand targeting of the folate receptor. Our drug delivery system consists of Pluronic-P105 micelles, targeted with folic acid moieties. A melanoma folate positive (FR+) (B16-F10), and a fibroblast folate negative (FR-) (NIH-3T3) cell lines are used to compare the cellular accumulation of a chemotherapeutic drug (Doxorubicin) when the delivery is mediated by folated Pluronic P105 micelles. In order to obtain a proper comparison, we corrected for the quenching of Doxorubicin by folic acid molecules and illustrated the significant effect of quenching on the analysis of similar systems. Results show an 80% increase in the accumulation of the antineoplastic agent in the FR+ cell line, when compared to the FR- cell line, thus providing evidence that the efficacy of Pluronic micelles, as drug delivery vehicles, can be enhanced via folic acid targeting.
机译:在本文中,我们报告了利用叶酸受体的配体靶向的潜在癌症药物递送系统。我们的药物输送系统由针对叶酸部分的Pluronic-P105胶束组成。当递送由叶酸介导时,使用黑素瘤叶酸阳性(FR +)(B16-F10)和成纤维细胞叶酸阴性(FR-)(NIH-3T3)细胞系来比较化疗药物(阿霉素)的细胞蓄积Pluronic P105胶束。为了获得适当的比较,我们校正了叶酸分子对阿霉素的淬灭作用,并说明了淬灭对相似系统分析的显著作用。结果显示,与FR-细胞系相比,FR +细胞系中抗肿瘤药的积累增加了80%,从而提供了证据,表明通过叶酸靶向可以提高Pluronic胶束作为药物传递载体的功效。 。

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