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γ-环糊精金属有机框架提高三氯蔗糖的热稳定性

Improvement in Thermal Stability of Sucralose by γ-Cyclodextrin Metal-Organic Frameworks.

作者信息

Lv Nana, Guo Tao, Liu Botao, Wang Caifen, Singh Vikaramjeet, Xu Xiaonan, Li Xue, Chen Dawei, Gref Ruxandra, Zhang Jiwen

机构信息

School of Pharmacy, Shenyang Pharmaceutical University, Shenyang, 110016, China.

Center for Drug Delivery System, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, No. 501 of Haike Road, Shanghai, 201210, China.

出版信息

Pharm Res. 2017 Feb;34(2):269-278. doi: 10.1007/s11095-016-2059-1. Epub 2016 Nov 28.

Abstract

PURPOSE

To explain thermal stability enhancement of an organic compound, sucralose, with cyclodextrin based metal organic frameworks.

METHODS

Micron and nanometer sized basic CD-MOFs were successfully synthesized by a modified vapor diffusion method and further neutralized with glacial acetic acid. Sucralose was loaded into CD-MOFs by incubating CD-MOFs with sucralose ethanol solutions. Thermal stabilities of sucralose-loaded basic CD-MOFs and neutralized CD-MOFs were investigated using thermogravimetric analysis (TGA), differential scanning calorimetry (DSC) and high performance liquid chromatography with evaporative light-scattering detection (HPLC-ELSD).

RESULTS

Scanning electron microscopy (SEM) and powder X-ray diffraction (PXRD) results showed that basic CD-MOFs were cubic crystals with smooth surface and uniform sizes. The basic CD-MOFs maintained their crystalline structure after neutralization. HPLC-ELSD analysis indicated that the CD-MOF crystal size had significant influence on sucralose loading (SL). The maximal SL of micron CD-MOFs (CD-MOF-Micro) was 17.5 ± 0.9% (w/w). In contrast, 27.9 ± 1.4% of sucralose could be loaded in nanometer-sized basic CD-MOFs (CD-MOF-Nano). Molecular docking modeling showed that sucralose molecules preferentially located inside the cavities of γ-CDs pairs in CD-MOFs. Raw sucralose decomposed fast at 90°C, with 86.2 ± 0.2% of the compound degraded within only 1 h. Remarkably, sucralose stability was dramatically improved after loading in neutralized CD-MOFs, with only 13.7 ± 0.7% degradation at 90°C within 24 h.

CONCLUSIONS

CD-MOFs efficiently incorporated sucralose and maintained its integrity upon heating at elevated temperatures.

摘要

目的

解释基于环糊精的金属有机框架对有机化合物三氯蔗糖热稳定性的增强作用。

方法

通过改进的气相扩散法成功合成了微米级和纳米级的碱性环糊精-金属有机框架(CD-MOFs),并用冰醋酸进一步中和。将三氯蔗糖与CD-MOFs在三氯蔗糖乙醇溶液中孵育,从而将三氯蔗糖负载到CD-MOFs中。使用热重分析(TGA)、差示扫描量热法(DSC)和蒸发光散射检测高效液相色谱法(HPLC-ELSD)研究负载三氯蔗糖的碱性CD-MOFs和中和后的CD-MOFs的热稳定性。

结果

扫描电子显微镜(SEM)和粉末X射线衍射(PXRD)结果表明,碱性CD-MOFs为表面光滑、尺寸均匀的立方晶体。中和后碱性CD-MOFs保持其晶体结构。HPLC-ELSD分析表明,CD-MOF晶体尺寸对三氯蔗糖负载量(SL)有显著影响。微米级CD-MOFs(CD-MOF-Micro)的最大SL为17.5±0.9%(w/w)。相比之下,纳米级碱性CD-MOFs(CD-MOF-Nano)中可负载27.9±1.4%的三氯蔗糖。分子对接模型表明,三氯蔗糖分子优先位于CD-MOFs中γ-环糊精对的腔内。未处理的三氯蔗糖在90°C时快速分解,仅1小时内就有86.2±0.2%的化合物降解。值得注意的是,负载到中和后的CD-MOFs中后,三氯蔗糖的稳定性显著提高,在90°C下24小时内仅有13.7±0.7%的降解。

结论

CD-MOFs有效地结合了三氯蔗糖,并在高温加热时保持其完整性。

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