College of Veterinary Medicine, Hebei Agricultural University, Baoding, Hebei 071000, China.
College of Veterinary Medicine, Hebei Agricultural University, Baoding, Hebei 071000, China.
Poult Sci. 2024 Jul;103(7):103768. doi: 10.1016/j.psj.2024.103768. Epub 2024 Apr 12.
Baicalein (BAI) is a natural flavonoid with antioxidant, antitumor and antibacterial properties. However, the bioavailability of BAI was limited due to low solubility. This study aims to improve the solubility of BAI through the amorphous solid dispersion (ASD) and evaluate changes in its pharmacokinetics and pharmacodynamics in Taihang chickens. Polyethylene caprolactam-polyvinyl acetate-polyethylene glycol grafted copolymer (Soluplus) was chosen as the carrier, and ASD was prepared by rotary evaporation and was characterized by powder X-ray diffractions (PXRD), differential scanning calorimetry (DSC) and fourier transform infrared spectroscopy (FT-IR). In vitro dissolution assays were used to screen the optimal ratio of drug to carrier, in vivo pharmacokinetic assays were conducted to investigate the promoting effect on the absorption. In addition, the effects of ASD on the growth performance, meat quality, antioxidant capacity and intestinal flora were investigated. ASD (1:9 and 2:8) did not exhibit crystal diffraction peaks of BAI in PXRD or endothermic peaks in DSC, indicating the successful preparation of ASD. The results of in vitro dissolution assay showed that the cumulative dissolution rate of ASD (2:8) within 600 min was 52.67%, which was 7.84-fold higher than BAI. The pharmacokinetic results showed that the peak concentration (C) and the area under the drug-time curve (AUC) of ASD (2:8) was (5.20 ± 0.82) μg/mL and (17.03 ± 0.67) μg·h/mL, which was 1.91 and 2.64-fold higher than BAI, respectively. Dietary supplementation of BAI and ASD could increase average daily gain (ADG), while decrease feed conversion ratio (FCR), but there was no significant difference (P > 0.05). The drip loss of BAIASD group was lower than BAI group (P < 0.05). In addition, the antioxidant capacity of Taihang chickens were enhanced, the diversity and the abundance of beneficial bacteria was improved. Results of BAI upon the dietary supplementation tested in Taihang chickens, after preparation of ASD, indicating a superior enhancement effect in growth performance, meat quality, antioxidant capacity and intestinal flora due to an improved solubility and optimized bioavailability.
白杨素（BAI）是一种具有抗氧化、抗肿瘤和抗菌特性的天然黄酮类化合物。然而，由于溶解度低，BAI 的生物利用度受到限制。本研究旨在通过无定形固体分散体（ASD）提高 BAI 的溶解度，并评估其在太行鸡中的药代动力学和药效学变化。选择聚己内酯-醋酸乙烯酯-聚乙二醇接枝共聚物（Soluplus）作为载体，通过旋转蒸发法制备 ASD，并通过粉末 X 射线衍射（PXRD）、差示扫描量热法（DSC）和傅里叶变换红外光谱（FT-IR）对其进行表征。体外溶出度试验筛选药物与载体的最佳比例，体内药代动力学试验研究其对吸收的促进作用。此外，还研究了 ASD 对生长性能、肉质、抗氧化能力和肠道菌群的影响。PXRD 中 ASD（1:9 和 2:8）未显示 BAI 的晶体衍射峰，DSC 中也没有吸热峰，表明 ASD 制备成功。体外溶出度试验结果表明，600 min 内 ASD（2:8）的累积溶出率为 52.67%，是 BAI 的 7.84 倍。药代动力学结果表明，ASD（2:8）的峰浓度（C）和药时曲线下面积（AUC）分别为（5.20±0.82）μg/mL 和（17.03±0.67）μg·h/mL，分别是 BAI 的 1.91 倍和 2.64 倍。饲粮中添加 BAI 和 ASD 可以提高平均日增重（ADG），降低饲料转化率（FCR），但差异不显著（P>0.05）。BAIASD 组的滴水损失低于 BAI 组（P<0.05）。此外，太行鸡的抗氧化能力增强，有益菌的多样性和丰度提高。结果表明，在太行鸡中饲粮添加 BAI 经 ASD 制备后，由于溶解度提高和生物利用度优化，生长性能、肉质、抗氧化能力和肠道菌群均有明显增强作用。
