冠醚/海藻酸钠包封给药策略中的姜黄素/nido-硼烷复合物具有 pH 值响应性释放和更强的体外抗肿瘤活性

IF 4.1 3区 工程技术 Q2 CHEMISTRY, APPLIED
Tiantian Chai , Mengtong Zhang , Shuo Wang , Jiankang Feng , Xibin Feng , Shihe Shao , Chichong Lu , Guofan Jin
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引用次数: 0

摘要

姜黄素具有出色的抗肿瘤活性,但其在生理 pH 值下的不稳定性、低生物利用度和靶向性差等问题限制了姜黄素进一步成为一种出色的抗癌药物。本研究制备了两种姜黄素/nido-硼烷荧光聚合物,即海藻酸钠包覆的姜黄素-硼烷-冠醚(SA-CBC)和姜黄素-硼烷-冠醚(CBC),其中SA-CBC具有更好的性能,是最有前途的抗肿瘤药物。冠醚/海藻酸钠给药策略可改善姜黄素的释放性能。Nido-硼烷增强了姜黄素的靶向性和对肿瘤细胞的抑制作用。经测试,SA-CBC 的荧光寿命为 4.72 ns,表明其具有良好的荧光特性。体外药物释放结果表明,所构建的给药系统能以可控的速率释放姜黄素。透射电子显微镜和粒度检测结果表明,SA-CBC封装良好,粒度小于200 nm,易于体内吸收。生物活性研究表明,SA-CBC 对肿瘤细胞具有很强的亲和力和抑制作用,抑制率可达 84.5%。总之,该研究为姜黄素抗癌药物的设计提供了一种创新方案,为开发更有效、副作用小的抗肿瘤药物奠定了基础。
本文章由计算机程序翻译,如有差异,请以英文原文为准。

Curcumin/nido-carborane complexes incorporated with crown ether/sodium alginate encapsulated drug delivery strategies exhibit pH-responsive release and enhanced in vitro anti-tumor activity

Curcumin/nido-carborane complexes incorporated with crown ether/sodium alginate encapsulated drug delivery strategies exhibit pH-responsive release and enhanced in vitro anti-tumor activity

Curcumin has excellent anti-tumor activity, but its instability at physiological pH, low bioavailability and poor targeting limit curcumin to further become an excellent anticancer drug. In this study, two curcumin/nido-carborane fluorescent polymers, curcumin-borane-crown ether coated by sodium alginate (SA-CBC) and curcumin-borane-crown ether (CBC), were prepared, and SA-CBC with better properties to be the most promising anti-tumor drugs. Crown ether/sodium alginate drug delivery strategies can improve the release property of curcumin. Nido-carborane enhances the targeting of curcumin and the inhibiting effect on tumor cells. After testing, the fluorescence lifetime of SA-CBC was 4.72 ns, indicating good fluorescence properties. In vitro drug release results showed that the constructed drug delivery system released curcumin at a controlled rate. The results of transmission electron microscopy and particle size showed that SA-CBC was well encapsulated, with a particle size of less than 200 nm, easy to be absorbed in vivo. Bioactivity studies showed that SA-CBC had a strong affinity and inhibiting effect on tumor cells, and the inhibition rate could reach 84.5 %. In conclusion, this study provides an innovative protocol for the design of curcumin anticancer drugs and lays the foundation for the development of more effective anti-tumor drugs with small side effects.

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来源期刊
Dyes and Pigments
Dyes and Pigments 工程技术-材料科学:纺织
CiteScore
8.20
自引率
13.30%
发文量
933
审稿时长
33 days
期刊介绍: Dyes and Pigments covers the scientific and technical aspects of the chemistry and physics of dyes, pigments and their intermediates. Emphasis is placed on the properties of the colouring matters themselves rather than on their applications or the system in which they may be applied. Thus the journal accepts research and review papers on the synthesis of dyes, pigments and intermediates, their physical or chemical properties, e.g. spectroscopic, surface, solution or solid state characteristics, the physical aspects of their preparation, e.g. precipitation, nucleation and growth, crystal formation, liquid crystalline characteristics, their photochemical, ecological or biological properties and the relationship between colour and chemical constitution. However, papers are considered which deal with the more fundamental aspects of colourant application and of the interactions of colourants with substrates or media. The journal will interest a wide variety of workers in a range of disciplines whose work involves dyes, pigments and their intermediates, and provides a platform for investigators with common interests but diverse fields of activity such as cosmetics, reprographics, dye and pigment synthesis, medical research, polymers, etc.
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