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首页> 外文期刊>Pharmaceutical development and technology >Hansen solubility parameters (HSP) for prescreening formulation of solid lipid nanoparticles (SLN): in vitro testing of curcumin-loaded SLN in MCF-7 and BT-474 cell lines
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Hansen solubility parameters (HSP) for prescreening formulation of solid lipid nanoparticles (SLN): in vitro testing of curcumin-loaded SLN in MCF-7 and BT-474 cell lines

机译：汉森溶解度参数（HSP）用于固体脂质纳米粒子（SLN）的预筛选配方：MCF-7和BT-474细胞系中姜黄素加载SLN的体外测试

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摘要

Curcumin, a phenolic compound from turmeric rhizome (Curcuma longa), has many interesting pharmacological effects, but shows very low aqueous solubility. Consequently, several drug delivery systems based on polymeric and lipid raw materials have been proposed to increase its bioavailability. Solid lipid nanoparticles (SLN), consisting of solid lipid matrix and a surfactant layer can load poorly water-soluble drugs, such as curcumin, deliver them at defined rates and enhance their intracellular uptake. In the present work, we demonstrate that, despite the drugs affinity to lipids frequently used in SLN production, the curcumin amount loaded in most SLN formulations may be too low to exhibit anticancer properties. The predictive curcumin solubility in solid lipids has been thoroughly analyzed by Hansen solubility parameters, in parallel with the lipid-screening solubility tests for a range of selected lipids. We identified the most suitable lipid materials for curcumin-loaded SLN, producing physicochemically stable particles with high encapsulation efficiency (>90%). Loading capacity of curcumin in SLN allowed preventing the cellular damage caused by cationic SLN on MCF-7 and BT-474 cells but was not sufficient to exhibit drugs anticancer properties. But curcumin-loaded SLN exhibited antioxidant properties, substantiating the conclusions that curcumins effect in cancer cells is highly dose dependent. ?2017 Informa UK Limited, trading as Taylor & Francis Group.
机译：姜黄素，来自姜黄根茎（Curcuma Longa）的酚类化合物，具有许多有趣的药理作用，但含有非常低的水溶性。因此，已经提出了基于聚合物和脂质原料的几种药物递送系统来增加其生物利用度。由固体脂质基质和表面活性剂层组成的固体脂质纳米颗粒（SLN）可以载有较差的水溶性药物，例如姜黄素，以定义的速率递送它们，并增强其细胞内摄取。在目前的工作中，我们证明，尽管对SLN生产经常使用的脂质的药物亲和力，但在大多数SLN制剂中负载的姜黄素可能太低，不能表现出抗癌性质。通过汉森溶解度参数，与脂筛分溶解度试验平行地通过脂筛分溶解度试验彻底分析固体脂质的预测姜黄素溶解度。我们鉴定了最合适的抗氟酸碱的SLN脂质材料，产生具有高封装效率的物理化学稳定的颗粒（> 90％）。在SLN中加载姜黄素的容量​​允许防止由MCF-7和BT-474细胞上阳离子SLN引起的细胞损伤，但不足以表现出抗癌性质。但是姜黄素加载的SLN表现出抗氧化性能，证实了癌细胞中姜黄素效应高度剂量依赖性的结论。 ？2017年Informa UK Limited，贸易为泰勒和弗朗西斯集团。

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