南美超级胎牛血清999尝鲜特惠
转染试剂低至5折
基质胶阶梯特惠
积分商城,好礼送不停
南美超级胎牛血清999尝鲜特惠
转染试剂低至5折
基质胶阶梯特惠
积分商城,好礼送不停

通过溶剂蒸发法制备的贝加莱因固体分散体可提高口服生物利用度,并缓解溃疡性结肠炎症状。

Baicalein solid dispersion prepared by solvent evaporation enhances oral bioavailability and alleviates ulcerative colitis

Xiali Wei, Xinyu Ji, Ziyang Li, Zixuan Guo, Yuxian Li, Qingri Jin

Journal:International Journal of Pharmaceutics-X

IF:7.9

DOI:10.1016/j.ijpx.2026.100602

PMID:

Published:2026-07-11

research field:分子生物学干细胞研究骨代谢细胞信号转导表观遗传学

Abstract

Baicalein (BAC) is a flavonoid compound known for its effectiveness in treating ulcerative colitis (UC). However, its clinical application is limited by poor water solubility, low stability, and low oral bioavailability. In this study, a baicalein solid dispersion (BAC-SD) was prepared using Polyvinylpyrrolidone (PVP) and hydroxypropyl methylcellulose (HPMC) as carriers via the solvent evaporation method. Scanning Electron Microscope (SEM), Powder X-Ray Diffraction 6000 diffractometer (PXRD), Differential Scanning Calorimetry (DSC), and Fourier Transform Infrared Spectroscopy (FT-IR) analyses confirmed the transition of BAC from a crystalline to an amorphous state. This transformation significantly improved the solubility, dissolution rate, and permeability of BAC. The in vitro dissolution results showed that the cumulative dissolution rate of BAC-SD reached 86.86% at 240 min, representing a 10.09-fold increase in solubility compared to BAC. In Caco-2 and MDCK cell models, the apparent permeability coefficient (Papp) of BAC-SD increased by 2.7- and 3.1-fold, respectively. Pharmacokinetic studies in rats demonstrated that the relative bioavailability of BAC-SD was 236.4% compared to BAC. In the DSS-induced UC mouse model, BAC-SD treatment alleviated UC by increasing colon length, improving pathological damage, and reducing both the Disease Activity Index (DAI) score and levels of inflammatory factors, including TNF-α, IL-1β, and IL-6. In conclusion, we successfully prepared BAC-SD and demonstrated that its therapeutic effect on UC is achieved by enhancing solubility, permeability, and oral bioavailability.

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