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姜黄素包载入层状双氢氧化物可提高其抗癌和抗寄生虫活性。

Encapsulation of curcumin into layered double hydroxides improve their anticancer and antiparasitic activity.

机构信息

Departamento de Química, Centro Universitario de Ciencias Exactas e Ingenierías, Universidad de Guadalajara, Guadalajara, México.

Departamento de Fisiología, Centro Universitario de Ciencias de la Salud, Universidad de Guadalajara, Guadalajara, México.

出版信息

J Pharm Pharmacol. 2020 Jul;72(7):897-908. doi: 10.1111/jphp.13266. Epub 2020 Apr 13.


DOI:10.1111/jphp.13266
PMID:32285474
Abstract

OBJECTIVES: Curcumin (CUR) has well-known activity against cancer cells and parasites; however, its applications are limited since this is an unstable molecule, which may suffer degradation by light and temperature, also, the low water solubility reduce its bioavailability. Layered double hydroxides (LDH) are well-known materials owing to the excellent anion exchange capacity, good biocompatibility and low toxicity. METHODS: Layered double hydroxides nanoparticles prepared with zinc and magnesium cations were used as a vehicle for CUR in Caco-2, Giardia lamblia and Entamoeba histolytica cultures. The physicochemical properties of Mg-LDH-CUR and Zn-LDH-CUR were characterized by scanning electron microscopy (SEM), Fourier transform infrared spectrometry (FTIR) and X-ray powder diffraction (XRD). Additionally, the load efficiency, release profiles and photostability of CUR were quantified by high-performance liquid chromatography (HPLC) and UV-Vis spectrometry. Then, Mg-LDH-CUR and Zn-LDH-CUR were tested on Caco-2, G. lamblia and E. histolytica cultures. KEY FINDINGS: The experiments demonstrated that Zn-LDH-CUR protects better against photodegradation by UV light, while Mg-LDH-CUR showed increased toxicity against Caco-2 cell, G. lamblia and E. histolytica, in comparison with free CUR. CONCLUSIONS: Layered double hydroxides are good vehicles to improve stability, resistance to degradation of CUR, also they are useful to improve solubility, provide a controlled release and improve the cytotoxic activity. Additionally, it was shown that the composition of the M cation of LDH affects its properties and structure and that this directly influences its biological activity. The findings are important to select the composition of the encapsulation vehicle for a specific activity.

摘要

目的:姜黄素(CUR)对癌细胞和寄生虫具有众所周知的活性;然而,由于其分子不稳定,可能会受到光和温度的降解,并且低水溶性降低其生物利用度,因此其应用受到限制。层状双氢氧化物(LDH)由于具有出色的阴离子交换能力、良好的生物相容性和低毒性而广为人知。

方法:使用锌和镁阳离子制备的层状双氢氧化物纳米颗粒作为 CUR 在 Caco-2、蓝氏贾第鞭毛虫和溶组织内阿米巴培养物中的载体。通过扫描电子显微镜(SEM)、傅里叶变换红外光谱(FTIR)和 X 射线粉末衍射(XRD)对 Mg-LDH-CUR 和 Zn-LDH-CUR 的物理化学性质进行了表征。此外,通过高效液相色谱(HPLC)和紫外可见光谱法对 CUR 的负载效率、释放曲线和光稳定性进行了定量。然后,在 Caco-2、G. lamblia 和 E. histolytica 培养物上测试了 Mg-LDH-CUR 和 Zn-LDH-CUR。

主要发现:实验表明,Zn-LDH-CUR 能更好地保护 CUR 免受紫外光的光降解,而与游离 CUR 相比,Mg-LDH-CUR 对 Caco-2 细胞、G. lamblia 和 E. histolytica 的毒性增加。

结论:层状双氢氧化物是提高 CUR 稳定性、抗降解性的良好载体,也有助于提高溶解度、提供控制释放并提高细胞毒性。此外,还表明 LDH 的 M 阳离子的组成会影响其性质和结构,从而直接影响其生物活性。这些发现对于选择特定活性的封装载体的组成很重要。

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Encapsulation of curcumin into layered double hydroxides improve their anticancer and antiparasitic activity.

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