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载 5-FU 和 DOX 的羧甲基淀粉双层氢氧化物纳米粒的体外性能评价。

Carboxymethyl starch encapsulated 5-FU and DOX co-loaded layered double hydroxide for evaluation of its in vitro performance as a drug delivery agent.

机构信息

Polymer Research Laboratory, Department of Organic and Biochemistry, Faculty of Chemistry, University of Tabriz, Tabriz, Iran.

Polymer Research Laboratory, Department of Organic and Biochemistry, Faculty of Chemistry, University of Tabriz, Tabriz, Iran; Research Center for Pharmaceutical Nanotechnology (RCPN), Tabriz University of Medical Science, Tabriz, Iran.

出版信息

Int J Biol Macromol. 2022 Mar 15;201:193-202. doi: 10.1016/j.ijbiomac.2021.12.181. Epub 2022 Jan 8.

DOI:10.1016/j.ijbiomac.2021.12.181
PMID:35007629
Abstract

Achieving a new oral drug delivery system with controlled drug release behavior is valuable in cancer therapy. Therefore, for the first time, doxorubicin (DOX) and 5-fluorouracil (5-Fu) were simultaneously co-loaded on the as-synthesized layered double hydroxides LDH(MgAl). The resulted system was encapsulated with carboxymethyl starch to improve its efficiency for colon cancer therapy. Several characterization techniques were used to evaluate the successful synthesis of the CMS@LDH(MgAl)@DOX,5-Fu microspheres. The scanning electron microscopy result showed that the size of prepared microspheres is about 72 μm. Additionally, the presence of one broad peak at 2θ ~ 20 of the X-ray diffraction spectrum approved its amorph nature. The drug release study showed a controlled release profile with ~22% of DOX and 29% of 5-Fu. In addition, the cell viability test outcome confirmed the sustained drug release pattern from CMS@LDH(MgAl)@DOX,5-Fu against the colon cancer cell line. The results suggest that the prepared microspheres are capable to operate as an acceptable formulation for oral co-drug delivery.

摘要

实现具有控制药物释放行为的新型口服药物输送系统在癌症治疗中具有重要价值。因此,我们首次将阿霉素(DOX)和 5-氟尿嘧啶(5-Fu)同时共负载于合成的层状双氢氧化物 LDH(MgAl)上。所得系统被羧甲基淀粉包封,以提高其用于结肠癌治疗的效率。使用了几种表征技术来评估成功合成了 CMS@LDH(MgAl)@DOX、5-Fu 微球。扫描电子显微镜结果表明,所制备的微球的尺寸约为 72 μm。此外,X 射线衍射光谱中 2θ 处的一个宽峰表明其非晶态性质。药物释放研究显示出一种控制释放的模式,其中约有 22%的 DOX 和 29%的 5-Fu 被释放。此外,细胞活力测试结果证实了 CMS@LDH(MgAl)@DOX、5-Fu 从微球中持续释放药物的模式,这对结肠癌细胞系有效。结果表明,所制备的微球可作为口服共药物递送的一种可接受的制剂。

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