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超顺磁聚硫醚酯纳米载药颗粒中 4-硝基查耳酮联合热疗的抗肿瘤活性。

Antitumor activity associated with hyperthermia and 4-nitrochalcone loaded in superparamagnetic poly(thioether-ester) nanoparticles.

机构信息

Department of Chemical Engineering and Food Engineering, Federal University of Santa Catarina, Florianopolis, Brazil.

Postgraduate Program in Health Science, University of Southern Santa Catarina, Criciúma, Brazil.

出版信息

J Biomater Sci Polym Ed. 2020 Oct;31(15):1895-1911. doi: 10.1080/09205063.2020.1782699. Epub 2020 Jul 3.

DOI:10.1080/09205063.2020.1782699
PMID:32552460
Abstract

The combination of hyperthermia and chemotherapy has a potential synergic effect in antitumor activity. The development of new biocompatible and biodegradable polymers to simultaneously encapsulate magnetic nanoparticles (MNPs) and antitumoral drugs offer new cancer treatment opportunities. Here, biodegradable and biocompatible poly(thioether-ester) (PTEe) was used to encapsulate MNPs and 4-nitrochalcone (4NC) using miniemulsification and solvent evaporation. The resulting hybrid particles (MNPs-4NC-PTEe) had nanometer-scale diameters, spherical morphology, negative surface charge, high encapsulation efficiency, and superparamagnetic properties. Results showed that 4NC release occurred through diffusion. Free 4NC and MNPs + 4NC-PTEe did not have any cytotoxic effect on erythrocytes and mouse embryonic fibroblast (NIH3T3) cells. 4NC antitumor activity was verified on human cervical cancer (HeLa) and melanoma (B16F10) cells. Cellular uptake of MNPs + 4NC-PTEe nanoparticles was higher in HeLa cells compared to B16F10 and NIH3T3 cells. The hyperthermia application (115 kHz-500 Oe) potentiated the 4NC effects on HeLa and B16F10 cells when MNPs + 4NC-PTEe nanoparticles were used, indicating more effective antitumor activity. We concluded that the use of MNPs + 4NC-PTEe nanoparticles associated with hyperthermia is a promising form of treatment for some types of cancers.

摘要

热疗与化疗联合具有抗肿瘤活性的潜在协同效应。开发新的生物相容性和可生物降解聚合物,同时包封磁性纳米颗粒(MNPs)和抗肿瘤药物,为癌症治疗提供了新的机会。在此,使用可生物降解和生物相容的聚(硫醚-酯)(PTEe)通过细乳液法和溶剂蒸发法来包封 MNPs 和 4-硝基查耳酮(4NC)。所得的混合粒子(MNPs-4NC-PTEe)具有纳米级粒径、球形形态、负表面电荷、高包封效率和超顺磁性。结果表明,4NC 通过扩散释放。游离 4NC 和 MNPs+4NC-PTEe 对红细胞和小鼠胚胎成纤维细胞(NIH3T3)无细胞毒性。4NC 的抗肿瘤活性在人宫颈癌(HeLa)和黑色素瘤(B16F10)细胞上得到验证。与 B16F10 和 NIH3T3 细胞相比,HeLa 细胞对 MNPs+4NC-PTEe 纳米粒子的细胞摄取更高。当使用 MNPs+4NC-PTEe 纳米粒子时,热疗(115 kHz-500 Oe)增强了 4NC 对 HeLa 和 B16F10 细胞的作用,表明具有更有效的抗肿瘤活性。我们得出结论,使用 MNPs+4NC-PTEe 纳米粒子联合热疗是治疗某些类型癌症的一种有前途的方法。

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