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基于原儿茶酸-锌层状氢氧化物纳米杂化物的具有控释性能的抗癌纳米递药系统。

Anticancer nanodelivery system with controlled release property based on protocatechuate-zinc layered hydroxide nanohybrid.

机构信息

Materials Synthesis and Characterization Laboratory, Institute of Advanced Technology (ITMA), Universiti Putra Malaysia.

Department of Biochemistry, Faculty of Biotechnology and Biomolecular Sciences, Universiti Putra Malaysia ; Laboratory of Vaccines and Immunotherapeutics, Institute of Bioscience, Universiti Putra Malaysia.

出版信息

Int J Nanomedicine. 2014 Jun 26;9:3137-49. doi: 10.2147/IJN.S59541. eCollection 2014.

Abstract

BACKGROUND

We characterize a novel nanocomposite that acts as an efficient anticancer agent.

METHODS

This nanocomposite consists of zinc layered hydroxide intercalated with protocatechuate (an anionic form of protocatechuic acid), that has been synthesized using a direct method with zinc oxide and protocatechuic acid as precursors.

RESULTS

The resulting protocatechuic acid nanocomposite (PAN) showed a basal spacing of 12.7 Å, indicating that protocatechuate was intercalated in a monolayer arrangement, with an angle of 54° from the Z-axis between the interlayers of the zinc layered hydroxide, and an estimated drug loading of about 35.7%. PAN exhibited the properties of a mesoporous type material, with greatly enhanced thermal stability of protocatechuate as compared to its free counterpart. The presence of protocatechuate in the interlayers of the zinc layered hydroxide was further supported by Fourier transform infrared spectroscopy. Protocatechuate was released from PAN in a slow and sustained manner. This mechanism of release was well represented by a pseudo-second order kinetics model. PAN has shown increased cytotoxicity compared to the free form of protocatechuic acid in all cancer cell lines tested. Tumor growth suppression was extensive, particularly in HepG2 and HT29 cell lines.

CONCLUSION

PAN is suitable for use as a controlled release formulation, and our in vitro evidence indicates that PAN is an effective anticancer agent. PAN may have potential as a chemotherapeutic drug for human cancer.

摘要

背景

我们描述了一种新型的纳米复合材料,它是一种有效的抗癌剂。

方法

这种纳米复合材料由锌层状氢氧化物插层原儿茶酸(原儿茶酸的阴离子形式)组成,是使用氧化锌和原儿茶酸作为前体制备的直接方法合成的。

结果

所得的原儿茶酸纳米复合材料(PAN)具有 12.7Å 的基面间距,表明原儿茶酸以单层排列方式被插层,层间的锌层状氢氧化物的 Z 轴之间的角度为 54°,估计药物负载量约为 35.7%。PAN 表现出介孔型材料的性质,与游离原儿茶酸相比,其热稳定性大大提高。傅里叶变换红外光谱进一步支持原儿茶酸存在于锌层状氢氧化物的层间。原儿茶酸从 PAN 中以缓慢和持续的方式释放。这种释放机制很好地由伪二阶动力学模型来表示。与游离原儿茶酸相比,PAN 在所有测试的癌细胞系中表现出更高的细胞毒性。肿瘤生长抑制作用广泛,特别是在 HepG2 和 HT29 细胞系中。

结论

PAN 适合用作控制释放制剂,我们的体外证据表明 PAN 是一种有效的抗癌剂。PAN 可能有作为人类癌症化疗药物的潜力。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/058a/4079826/899fcef939a8/ijn-9-3137Fig1.jpg

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