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酥油作为一种治疗给药系统。

Ghee Butter as a Therapeutic Delivery System.

作者信息

Balasubramanian Kishore, Evangelopoulos Michael, Brown Brandon S, Parodi Alessandro, Celia Christian, Yazdi Iman K, Tasciotti Ennio

出版信息

J Nanosci Nanotechnol. 2017 Feb;17(2):977-82. doi: 10.1166/jnn.2017.12623.

Abstract

Solid lipid nanoparticles carrying a chemotherapeutic payload (i.e., temozolomide, TMZ) were synthesized using ghee, a clarified butter commonly used in traditional medicine and food products. Ghee solid lipid nanoparticles (GSLN) were characterized through dynamic light scattering, scanning electron microscopy, and UV-visible spectrometry. Formulations were generated with varying ratios of surfactant to lipid, resulting in a maximum TMZ entrapment efficiency of ˜70%. Optimal formulations were found to have an average size and polydispersity of ˜220 nm and 0.340, respectively. Release kinetics revealed TMZ-loaded GSLN (TMZ@GSLN) retained 10% of its pay-load at 2 h with ˜53% released in 5 h. Metabolic activity on human umbilical vein endothelial cells (HUVEC) revealed GSLN treatment resulted in an increase in viability following 3 d while treatment of glioblastoma LN-229 cells with TMZ@GSLN resulted in a significant decrease. Evaluation of diffusion of TMZ across a reconstructed HUVEC monolayer demonstrated TMZ@GSLN resulted in a significantly higher diffusion of drug when compared to free TMZ. This data suggests GSLN pose a promising delivery vehicle for TMZ-based therapeutics. Collectively, this data demonstrates GSLN exhibit favorable drug carrier properties with anti-proliferative properties in glioblastoma cancer cells.

摘要

携带化疗药物(即替莫唑胺,TMZ)的固体脂质纳米粒是使用酥油合成的,酥油是一种常用于传统医学和食品的澄清黄油。通过动态光散射、扫描电子显微镜和紫外可见光谱对酥油固体脂质纳米粒(GSLN)进行了表征。制备了具有不同表面活性剂与脂质比例的制剂,导致最大的替莫唑胺包封效率约为70%。发现最佳制剂的平均尺寸和多分散性分别约为220nm和0.340。释放动力学表明,负载替莫唑胺的GSLN(TMZ@GSLN)在2小时时保留了10%的负载量,在5小时内释放了约53%。对人脐静脉内皮细胞(HUVEC)的代谢活性研究表明,GSLN处理3天后细胞活力增加,而用TMZ@GSLN处理胶质母细胞瘤LN-229细胞则导致细胞活力显著下降。评估替莫唑胺在重建的HUVEC单层上的扩散情况表明,与游离替莫唑胺相比,TMZ@GSLN导致药物扩散显著更高。这些数据表明GSLN是基于替莫唑胺的治疗药物的一种有前景的递送载体。总体而言,这些数据表明GSLN具有良好的药物载体特性,并在胶质母细胞瘤癌细胞中具有抗增殖特性。

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