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甘草素-羟丙基-β-环糊精包合物的制备、表征、生物利用度及抗肿瘤活性评价。

Liquiritin-Hydroxypropyl-Beta-Cyclodextrin Inclusion Complex: Preparation, Characterization, Bioavailability and Antitumor Activity Evaluation.

机构信息

Department of Pharmaceutics, School of Pharmacy, Centre for Nano Drug/Gene Delivery and Tissue Engineering, Jiangsu University, Zhenjiang 212013, People's Republic of China.

Department of Biochemistry and Forensic Science, School of Chemical and Biochemical Sciences, C. K. Tedam University of Technology, and Applied Sciences, Navrongo, Ghana.

出版信息

J Pharm Sci. 2022 Jul;111(7):2083-2092. doi: 10.1016/j.xphs.2022.03.021. Epub 2022 Mar 31.

Abstract

The pharmacological activities of liquiritin (LT) are greatly limited by its insolubility and low oral absorption. The purpose of this study was to prepare LT-hydroxypropyl-beta-cyclodextrin inclusion complex (LT-HP-β-CD) to increase water solubility, oral bioavailability and antitumor effect of LT. Herein, saturated aqueous solution method was applied to prepare the LT-HP-β-CD prior to characterization via scanning electron microscope (SEM), infrared radiation (IR) spectroscopy, X-ray diffraction analysis (XRD), and differential scanning calorimetry (DSC). Also, in vitro release and in vivo pharmacokinetics were evaluated. Moreover, the anti-tumor activity of the formulation was investigated in the A549 lung cancer cells. The results of SEM, IR, XRD and DSC showed that LT-HP-β-CD was successfully formulated. In vitro release and oral bioavailability of LT-HP-β-CD compared with the free LT was significantly higher. Successfully, antitumor effect of LT was remarkably enhanced by the preparation of LT-HP-β-CD. Altogether, the LT-HP-β-CD represents a potential carrier for enhancing the water solubility and oral bioavailability of LT coupled with antitumor activity enhancement.

摘要

甘草素(LT)的药理学活性受到其不溶性和低口服吸收的极大限制。本研究旨在制备 LT-羟丙基-β-环糊精包合物(LT-HP-β-CD),以提高 LT 的水溶性、口服生物利用度和抗肿瘤作用。在此,采用饱和水溶液法制备 LT-HP-β-CD,然后通过扫描电子显微镜(SEM)、红外辐射(IR)光谱、X 射线衍射分析(XRD)和差示扫描量热法(DSC)进行表征。此外,还评估了体外释放和体内药代动力学。此外,还研究了该制剂在 A549 肺癌细胞中的抗肿瘤活性。SEM、IR、XRD 和 DSC 的结果表明 LT-HP-β-CD 已成功制备。与游离 LT 相比,LT-HP-β-CD 的体外释放和口服生物利用度显著提高。LT-HP-β-CD 的制备显著增强了 LT 的抗肿瘤作用。总之,LT-HP-β-CD 代表了一种提高 LT 水溶性和口服生物利用度并增强抗肿瘤活性的潜在载体。

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