School of Pharmacy, College of Pharmacy, Lanzhou University, No.199, Donggang West Road, Lanzhou, 730000, China.
Eur J Drug Metab Pharmacokinet. 2022 Sep;47(5):677-686. doi: 10.1007/s13318-022-00783-8. Epub 2022 Jul 5.
Oral colon-targeted gel beads containing isoliquiritigenin (ISL) were successfully designed in our study. In order to further explore the targeting of the colon by the gel beads, a systematic study of their in vivo pharmacokinetics and colon targeting was performed in mice.
Eighteen male mice were included in this study. The mice were separated into six groups at random. We collected blood, stomach, duodenum, jejunum, ileum, and colon tissues at 2, 4, 6, 8, 12, and 24 h after oral administration of gel beads containing isoliquiritigenin at a dose of 20 mg/kg. Gel beads in tissues were recorded and taken out to observe their swelling and erosion. The total ISL concentrations in different tissues and gel beads were analyzed by high-performance liquid chromatography.
All gel beads reached the upper part of the stomach at 2 h with no obvious swelling. Most of the gel beads were still in the lower part of stomach, while a small amount had reached the small intestine at 4 h. A few gel beads reached the colon and swelled at 6 h. Furthermore, the gel beads in the colon were swollen and erosive at 8 h. Meanwhile, the plasma ISL concentration could be detected, which indicated that the ISL in the gel beads was absorbed. At 12 h, the gel beads were almost dissolved and the plasma concentration was 8.33 times that at 8 h. At 24 h, the gel beads had completely disappeared, and the plasma concentration was 2.55 times that at 12 h.
The gel beads containing ISL are a sustained, controlled, and colon-targeting delivery system that can alter the ISL distribution in the gastrointestinal tract.
本研究成功设计了含有异甘草素的口服结肠靶向凝胶珠。为了进一步探讨凝胶珠对结肠的靶向作用，我们在小鼠体内进行了系统的药代动力学和结肠靶向研究。
本研究纳入 18 只雄性小鼠，随机分为 6 组。在口服 20mg/kg 剂量的含异甘草素凝胶珠后，分别于 2、4、6、8、12 和 24h 采集血、胃、十二指肠、空肠、回肠和结肠组织。记录组织中的凝胶珠并取出观察其膨胀和侵蚀情况。采用高效液相色谱法分析不同组织和凝胶珠中的总异甘草素浓度。
所有凝胶珠在 2h 时均到达胃上部，无明显肿胀。大多数凝胶珠仍在胃下部，而少量已在 4h 时到达小肠。少数凝胶珠在 6h 时到达结肠并膨胀。此外，在 8h 时，结肠中的凝胶珠膨胀和侵蚀。同时，可检测到凝胶珠中异甘草素的血浆浓度，表明凝胶珠中的异甘草素被吸收。在 12h 时，凝胶珠几乎溶解，血浆浓度是 8h 时的 8.33 倍。在 24h 时，凝胶珠完全消失，血浆浓度是 12h 时的 2.55 倍。
含异甘草素的凝胶珠是一种持续、控制和结肠靶向的给药系统，可改变胃肠道中异甘草素的分布。
