首页> 美国卫生研究院文献>Drug Delivery >Hyaluronic acid-modified didecyldimethylammonium bromide/ d-a-tocopheryl polyethylene glycol succinate mixed micelles for delivery of baohuoside I against non-small cell lung cancer: in vitro and in vivo evaluation
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Hyaluronic acid-modified didecyldimethylammonium bromide/ d-a-tocopheryl polyethylene glycol succinate mixed micelles for delivery of baohuoside I against non-small cell lung cancer: in vitro and in vivo evaluation

机译:透明质酸改性的小二甲基二甲基溴铵/ D-α-生育基聚乙基二醇琥珀酸盐混合胶束用于递送保福苷I对抗非小细胞肺癌:体外和体内评价

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摘要

Baohuoside I is an effective but a poorly soluble antitumor drug. In this study, we prepared baohuoside I-loaded mixed micelles with didecyldimethylammonium bromide (DDAB) and d-a-tocopheryl polyethylene glycol succinate (TPGS) (DTBM) and active targeting mixed micelles (HDTBM) with hyaluronic acid (HA) as the targeting ligand on the surface of the mixed micelles. We performed a systematic comparative evaluation of the antiproliferative effect, cellular uptake, antitumor efficacy, and in vivo tumor targeting of these micelles using A549 cells. HDTBM showed improved cellular uptake and had a greater hypersensitizing effect on A549 cell lines than baohuoside I; half-maximal inhibitory concentration (IC50) was 8.86 versus 20.42 μg/mL, respectively. Results of the antitumor efficacy study and the imaging study for in vivo targeting showed that the mixed-micelle formulation had higher antitumor efficacy and achieved effective and targeted drug delivery. Therefore, our results indicate that HA/baohuoside I-M may be used as a potential antitumor formulation.
机译:宝泉I是一种有效而是一种可溶性抗肿瘤药物。在这项研究中,我们用DIDECYLDIMED甲基溴(DDAB)和DA-生育基聚乙二醇琥珀酸盐(DTBS)(DTBM)和具有透明质酸(HA)的活性靶向混合胶束(HDTBM)作为靶向配体的活性靶向混合胶束(HDTBM)。混合胶束的表面。我们使用A549细胞进行了对抗增殖效应,细胞吸收,抗肿瘤效力的系统性比较评估,细胞吸收,抗肿瘤功效,以及这些胶束的体内肿瘤靶向。 HDTBM显示出改善的细胞摄取,对A549细胞系具有比宝泉I的更大的过敏效果;半最大抑制浓度(IC 50)分别为8.86与20.42μg/ ml。抗肿瘤功效研究的结果及体内靶向的成像研究表明,混合胶束配方具有较高的抗肿瘤功效,并实现有效和靶向药物递送。因此,我们的结果表明HA / Baohuoside I-M可以用作潜在的抗肿瘤制剂。

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