水溶性对硫壬基芳烃[4]的柚皮素增溶及pH依赖性释放特性

IF 2.1 4区化学 Q3 CHEMISTRY, MULTIDISCIPLINARY

Supramolecular Chemistry Pub Date : 2021-09-02 DOI:10.1080/10610278.2022.2061352

T. Khokhar, Fakhar N. Memon, S. S. Memon, A. Memon, A. A. Bhatti, S. Memon

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引用次数: 3

摘要

摘要:本研究报道了p-磺atocalix[4]芳烃(p-SCX4)对柚皮素(Naringenin, NAR)的增溶特性，通过在生理pH下形成包合物，随后在酸性pH下释放，从而改善药代动力学特性和生物利用度。通过紫外可见光谱和傅里叶变换红外光谱等光谱技术证实柚皮素与p -SCX4的络合作用。通过HPLC-DAD分析柚皮素(1)、p-SCX4(2)和p-SCX4/NAR(3)进一步确定络合物的形成。采用Job’s plot法和Benesi-Hildebrand方程计算络合物的化学计量。用Higuchi和Connors法测定柚皮素的溶解度。结果表明，药物与p-SCX4呈1:1的化学计量关系。溶解系数提高10倍以上。考察了该配合物在不同pH值下的药物溶出/释放行为，在pH = 3.5时，在220 min的时间间隔内观察到最大%释放量。图形抽象

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Naringenin solubilizing and pH dependent releasing properties of water soluble p-sulphonatocalix[4]arene

ABSTRACT This study reports the solubilizing properties of p-sulphonatocalix[4]arene ( p-SCX4) towards Naringenin (NAR) to improve pharmacokinetic characteristics and bioavailability by forming inclusion complex at physiological pH and subsequent release at acid pH values. The complexation of naringenin with p -SCX4 was confirmed through spectroscopic techniques such as UV–visible spectroscopy and Fourier transform infrared spectroscopy. Complex formation was further confirmed through HPLC-DAD analysis by identification of naringenin (1), p-SCX4 (2), and p-SCX4/NAR (3). Job’s plot method and Benesi–Hildebrand equation was used to find the stoichiometry of complex. Solubility of naringenin was determined by Higuchi and Connors method. Results show that there is 1:1 stoichiometry between drug and p-SCX4. The solubility factor was increase up to 10 folds. The drug dissolution/releasing behaviour of the complex was examined at different pH values, and maximum % release amount was observed at pH = 3.5 within time interval up to 220 minutes. Graphical abstract

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来源期刊

Supramolecular Chemistry 化学-化学综合

CiteScore

3.60

自引率

3.00%

发文量

审稿时长

2.7 months

期刊介绍： Supramolecular Chemistry welcomes manuscripts from the fields and sub-disciplines related to supramolecular chemistry and non-covalent interactions. From host-guest chemistry, self-assembly and systems chemistry, through materials chemistry and biochemical systems, we interpret supramolecular chemistry in the broadest possible sense. Interdisciplinary manuscripts are particularly encouraged. Manuscript types include: high priority communications; full papers; reviews, and; Methods papers, techniques tutorials highlighting procedures and technologies that are important to the field. We aim to publish papers in a timely fashion and as soon as a paper has been accepted and typeset it will be published in electronic form on the Latest articles section of the website. The two most important review criteria are that the paper presents high-quality work that fits generally into the broad spectrum of activities in the supramolecular chemistry field. Under normal circumstances, Supramolecular Chemistry does not consider manuscripts that would be more suitable in a highly specialized journal. This includes, but is not limited to, those based mostly or exclusively on topics such as solid state/X-ray structures, computational chemistry, or electrochemistry. . The two most important review criteria are that the paper presents high-quality work that fits generally into the broad spectrum of activities in the supramolecular chemistry field.