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Mg/Al- 和 Zn/Al 层状双氢氧化物-培哚普利厄贝沙坦纳米复合材料抑制血管紧张素转换酶的比较研究。

Comparative study of Mg/Al- and Zn/Al-layered double hydroxide-perindopril erbumine nanocomposites for inhibition of angiotensin-converting enzyme.

机构信息

Department of Chemistry, Faculty of Science, Universiti Putra Malaysia, Serdang, Selangor, Malaysia.

出版信息

Int J Nanomedicine. 2012;7:4251-62. doi: 10.2147/IJN.S32267. Epub 2012 Aug 3.

Abstract

The intercalation of a drug active, perindopril, into Mg/Al-layered double hydroxide for the formation of a new nanocomposite, PMAE, was accomplished using a simple ion exchange technique. A relatively high loading percentage of perindopril of about 36.5% (w/w) indicates that intercalation of the active took place in the Mg/Al inorganic interlayer. Intercalation was further supported by Fourier transform infrared spectroscopy, and thermal analysis shows markedly enhanced thermal stability of the active. The release of perindopril from the nanocomposite occurred in a controlled manner governed by pseudo-second order kinetics. MTT assay showed no cytotoxicity effects from either Mg/Al-layered double hydroxide or its nanocomposite, PMAE. Mg/Al-layered double hydroxide showed angiotensin-converting enzyme inhibitory activity, with 5.6% inhibition after 90 minutes of incubation. On incubation of angiotensin-converting enzyme with 0.5 μg/mL of the PMAE nanocomposite, inhibition of the enzyme increased from 56.6% to 70.6% at 30 and 90 minutes, respectively. These results are comparable with data reported in the literature for Zn/Al-perindopril.

摘要

药物活性成分培哚普利被插入到 Mg/Al 层状双氢氧化物中,形成一种新的纳米复合材料 PMAE,该过程采用了一种简单的离子交换技术。培哚普利的负载量相对较高,约为 36.5%(w/w),表明活性成分在 Mg/Al 无机层间发生了插层。傅里叶变换红外光谱进一步证实了插层的发生,热分析表明活性成分的热稳定性显著增强。培哚普利从纳米复合材料中的释放以伪二级动力学控制的方式进行。MTT 测定表明,Mg/Al 层状双氢氧化物或其纳米复合材料 PMAE 均无细胞毒性作用。Mg/Al 层状双氢氧化物具有血管紧张素转化酶抑制活性,孵育 90 分钟后抑制率为 5.6%。当将血管紧张素转化酶与 0.5μg/mL 的 PMAE 纳米复合材料孵育时,酶的抑制率分别在 30 分钟和 90 分钟时从 56.6%增加到 70.6%。这些结果与文献中报道的 Zn/Al-培哚普利的数据相当。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4780/3418079/05cd86ff406f/ijn-7-4251f1.jpg

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