STAT3 抑制剂固体脂质纳米载体系统的配方优化,以提高其在三阴性乳腺癌细胞中的活性。

Formulation-optimization of solid lipid nanocarrier system of STAT3 inhibitor to improve its activity in triple negative breast cancer cells.

机构信息

a Department of Pharmacology, JSS College of Pharmacy, Ooty (Constituent College) , JSS Academy of Higher Education and Research , Mysuru , India.

出版信息

Drug Dev Ind Pharm. 2019 Feb;45(2):304-313. doi: 10.1080/03639045.2018.1539496. Epub 2018 Nov 8.

Abstract

In the present study, solid lipid nanoparticles (SLNs) have been formulated as a carrier system for effective intracellular delivery of STAT3 inhibitor, niclosamide (Niclo) to triple negative breast cancer (TNBC) cells. Emulsification-solvent evaporation method was employed in formulation of Niclo-loaded SLNs (Niclo-SLNs). The formula of Niclo-SLN was optimized by Box-Behnken design and characterized for their shape, size, and surface charge. The in vitro anti-cancer efficacy of Niclo-SLNs was studied in TNBC cells. The prepared Niclo-SLNs were found to be spherical with the particle size of 112.18 ± 1.73 nm and zetapotential of 23.8 ± 2.7 mV. In the in vitro anticancer study the Niclo SLNs show a better cytotoxicity than the naïve Niclo, which is attributed to improved cell uptake of SLN formulation. In conclusion, the results of the present study demonstrate that the formulation of Niclo as SLNs will improve the anticancer efficacy against TNBC.

摘要

在本研究中,固体脂质纳米粒(SLN)被制成一种载体系统,用于将 STAT3 抑制剂尼氯硝唑(Niclo)有效递送至三阴性乳腺癌(TNBC)细胞内。采用乳化-溶剂蒸发法制备尼氯硝唑负载的 SLN(Niclo-SLN)。采用 Box-Behnken 设计对 Niclo-SLN 的配方进行优化,并对其形状、大小和表面电荷进行了表征。研究了尼氯硝唑 SLN 在 TNBC 细胞中的体外抗癌功效。所制备的尼氯硝唑 SLN 呈球形,粒径为 112.18±1.73nm,Zeta 电位为 23.8±2.7mV。在体外抗癌研究中,尼氯硝唑 SLN 表现出比天然尼氯硝唑更好的细胞毒性,这归因于 SLN 制剂改善了细胞摄取。总之,本研究结果表明,将尼氯硝唑制成 SLN 将提高对 TNBC 的抗癌功效。

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