关于合成索拉非尼与 2-羟丙基-β-环糊精的复合物以增强药物抗癌活性的研究

IF 2 4区化学 Q3 CHEMISTRY, MULTIDISCIPLINARY

Pure and Applied Chemistry Pub Date : 2024-03-25 DOI:10.1515/pac-2024-0024

Van Cuong Bui, Thi Lan Pham, Thi Lam Nguyen, Thi Kim Chinh Tran, Thi My Hanh Le Le, Xuan Minh Vu, Irina M. Le-Deygen, Chau Anh Nguyen, Thanh Tung Mai, Raa Khimi Shuib

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引用次数: 0

摘要

本研究旨在合成索拉非尼（Sorafenib，Sor）与羟丙基-β-环糊精（HPβCD，Hydroxypropyl-β-cyclodextrin）的包涵复合物（简称[Sor-HPβCD]）。Sor 与 HPβCD 的复合物是在 H2O-DMSO 混合溶剂中合成的，其中 DMSO 的体积分数为 80%。傅立叶变换红外光谱（FTIR）、电导率稳定分析（DSC）和紫外可见光分析的结果表明，络合物的形成是成功的：络合物形成后，Sor 结合的一些特征峰的强度降低，表明部分客体分子进入了 HPβCD 分子的空腔。DSC 分析结果进一步证实了这一点，该分析表明复合物的结晶形态已转变为无定形形态。相溶解度图研究也表明，络合物形成后，Sor 的溶解度显著增加，约为纯 Sor 的 7 倍。在水环境中进行的细胞生长抑制活性测试结果表明，复合物抑制 Hep-G2 细胞生长的 IC50 值为 62.4 μg/mL，而纯 Sor 因几乎不溶于水而没有活性。

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Study on synthesizing the complex of sorafenib with 2-hydroxypropyl-β-cyclodextrin to enhance the anticancer activity of the drug substance

This study aims to synthesize inclusion complex derived from sorafenib (Sor) and hydroxypropyl-β-cyclodextrin (HPβCD) (denoted as [Sor-HPβCD]). The complex of Sor with HPβCD has been synthesized in a mixed solvent of H2O-DMSO, with a DMSO volume fraction of 80 %. The results of FTIR, DSC, and UV–Vis analysis have demonstrated the success of complex formation: the intensity of some characteristic peaks for the Sor binding decreased after complex formation, indicating that a part of the guest molecule has entered the cavity of the HPβCD molecule. This is further supported by the DSC analysis results, showing the transformation of the complex’s crystalline form to an amorphous form. The phase solubility diagram study also indicates that the solubility of Sor significantly increases, approximately 7 times higher than pure Sor, after complex formation. The results of the cell growth inhibition activity test in a water environment show that the complex inhibits the growth of Hep-G2 cells with an IC50 value of 62.4 μg/mL, while pure Sor does not exhibit activity as it is practically insoluble in water.

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来源期刊

Pure and Applied Chemistry 化学-化学综合

CiteScore

4.00

自引率

0.00%

发文量

审稿时长

3-8 weeks

期刊介绍： Pure and Applied Chemistry is the official monthly Journal of IUPAC, with responsibility for publishing works arising from those international scientific events and projects that are sponsored and undertaken by the Union. The policy is to publish highly topical and credible works at the forefront of all aspects of pure and applied chemistry, and the attendant goal is to promote widespread acceptance of the Journal as an authoritative and indispensable holding in academic and institutional libraries.