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Development and In Vitro Characterization of Paclitaxel Loaded Solid Lipid Nanoparticles

机译:紫杉醇装载固体脂质纳米粒子的开发和体外表征

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Background: Paclitaxel (PTX) is a potent anticancer drug which is highly effective against several cancers. Solid lipid nanoparticles (SLNs) loaded with anticancer drugs can enhance its toxicity against tumor cells at low concentrations. Objective: To develop and characterize SLNs of PTX (PSLN) to enhance its toxicity against cancerous cells. Method: The solubility of PTX was screened in various lipids. Solid lipid nanoparticles of PTX (PSLN) were developed by hot homogenization method using Cutina HR and Ge- lucire 44/14 as lipid carriers and Solutol HS 15 as a surfactant. PSLNs were characterized for size, morphology, zeta potential, entrapment efficiency, physical state of the drug and in vitro release profile in 7.4 pH phosphate buffer saline (PBS). The ability of PTX to enhance toxicity towards cancerous cells was tested by performing cytoxicity assay in MCF7 cell line. Results: Solubility studies of PTX in lipids indicated better solubility when Cutina HR and Gelucire 44/14 were used. PSLNs were found to possess a neutral zeta potential with a size range of 155.4 ± 10.7 nm to 641.9 ± 4.2 nm. In vitro release studies showed a sustained release profile for PSLN over a period of 48 hours. SLNs loaded with PTX were found to be more toxic in killing MCF7 cells at a lower concentration than the free PTX.
机译:背景:紫杉醇(PTX)是一种有效的抗癌药,对几种癌症非常有效。装载抗癌药物的固体脂质纳米颗粒(SLNS)可以在低浓度下提高对肿瘤细胞的毒性。目的:开发和表征PTX(PSLN)的SLN,以增强癌细胞的毒性。方法:在各种脂质中筛选PTX的溶解度。通过使用Cutina HR和Ge-Lucire 44/14作为脂质载体和Solutol HS 15作为表面活性剂,通过热均化方法进行PTX(PSLN)的固体脂质纳米颗粒。 PSLNS的特征在于7.4 pH磷酸盐缓冲盐水(PBS)中的尺寸,形态,Zeta电位,夹带效率,药物的物理状态和体外释放曲线。通过在MCF7细胞系中进行细胞毒性测定来测试PTX对癌细胞增强毒性的能力。结果:当使用Cutina HR和Gelucire 44/14时,脂质中PTX的溶解度研究表明了较好的溶解度。发现PSLNS具有中性Zeta电位,尺寸范围为155.4±10.7nm至641.9±4.2nm。体外释放研究在48小时的时间内显示出PSLN的持续释放曲线。发现用PTX加载的SLNS在终浓度低于游离PTX时杀死MCF7细胞更大。

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