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载他莫昔芬的纳米结构脂质载体作为药物传递系统:特性描述、稳定性评估和细胞毒性。

Tamoxifen-loaded nanostructured lipid carrier as a drug delivery system: characterization, stability assessment and cytotoxicity.

机构信息

Institute of Biosciences, Universiti Putra Malaysia, 43400 UPM Serdang, Selangor Darul Ehsan, Malaysia.

出版信息

Colloids Surf B Biointerfaces. 2013 Dec 1;112:393-9. doi: 10.1016/j.colsurfb.2013.08.009. Epub 2013 Aug 18.

Abstract

Cancer nanotherapeutics is beginning to overwhelm the global research and viewed to be the revolutionary treatment regime in the medical field. This investigation describes the development of a stable nanostructured lipid carrier (NLC) system as carrier for Tamoxifen (TAM). The TAM-loaded NLC (TAM-NLC) developed with 200mg of TAM showed a spherical particle with the size of 46.6nm, polydispersity index of 0.267, entrapment efficiency of 99.74% and with the zeta potential of -23.78mV. Besides, the equivalent cytotoxicity of TAM and TAM-NLC to human (MCF-7) and mice (4T1) mammary breast cancer cell lines were observed. Incubating the formulation at the physiological pH resulted into reduced Ostwald ripening rate but without any significant change in the absorptivity. When coupled with the measurements of zeta potential and Ostwald ripening rate, the absorbance assay may be used to predict the long-term stability of drug-loaded nanoparticle formulations. The results of the study also suggest that TAM-NLC is a promising drug delivery system for breast cancer therapy. This is the first encouraging report on the in vitro effect of TAM-NLC against human and mouse mammary adenocarcinoma cell lines.

摘要

癌症纳米治疗学正在全球范围内兴起,被视为医学领域的革命性治疗方法。本研究描述了一种稳定的纳米结构脂质载体(NLC)系统作为他莫昔芬(TAM)载体的开发。载有 TAM 的 NLC(TAM-NLC)的开发,使用了 200mg 的 TAM,显示出粒径为 46.6nm 的球形颗粒,多分散指数为 0.267,包封效率为 99.74%,zeta 电位为-23.78mV。此外,观察了 TAM 和 TAM-NLC 对人(MCF-7)和小鼠(4T1)乳腺癌细胞系的等效细胞毒性。在生理 pH 下孵育制剂会降低奥斯特瓦尔德熟化速率,但对吸光度没有任何显著影响。当与 zeta 电位和奥斯特瓦尔德熟化速率的测量相结合时,吸光度测定法可用于预测载药纳米颗粒制剂的长期稳定性。研究结果还表明,TAM-NLC 是一种有前途的乳腺癌治疗药物递送系统。这是关于 TAM-NLC 对人源和鼠源乳腺癌细胞系的体外作用的首次令人鼓舞的报告。

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