新型固体自乳化药物输送系统可增强cabazitaxel口服生物可用性
Xianxiong Sun1, Gaoshuai Lv1, Jian Xiong1
1Department of Pharmaceutics, School of Pharmacy, Shenyang Pharmaceutical University, Shenyang 110016, Liaoning, China.
International journal of pharmaceutics
|February 16, 2024
概括
一种新的cabazitaxel固体自乳化药物递送系统 (CTX S-SEDDS) 提高了口服生物利用性. 这种新系统克服了传统的自我乳化药物输送系统 (SEDDS) 的局限性,以改善卡巴西塔塞尔的输送.
科学领域:
- 制药科学 制药科学
- 药物输送系统 药物输送系统
- 纳米技术纳米技术
背景情况:
- 卡巴西塔克塞尔是一种水溶性较差的药物,口服生物利用性有限.
- 传统的自我乳化药物输送系统 (SEDDS) 在稳定性和处理方面面临挑战.
- 需要改善cabazitaxel的口服输送系统.
研究的目的:
- 开发一种新的cabazitaxel固体自乳化药物递送系统 (CTX S-SEDDS).
- 克服传统SEDDS的局限性.
- 为了提高cabazitaxel的口服生物可用性.
主要方法:
- 使用溶剂蒸发和液体-固体压缩开发CTX S-SEDDS.
- 优化表面活性剂 (Tween 80),油 (Tricaprylin,糖单酸盐) 的比例.
- 选择载体 (Syloid XDP3050) 和涂层 (Syloid 244FP) 材料.
- 在小鼠体外表征和体内药理动力学研究.
主要成果:
- 优化的配方实现了颗粒尺寸为140.87nm,乳化时间短,药物负载高 (50mg·g-1).
- CTX S-SEDDS表现出卓越的流动性,可表化性和复制性质.
- 在体内研究显示,CTX S-SEDDS (17.27%) 的绝对生物可用性与cabazitaxel溶液 (1.69%) 相比显著提高.
- 淋巴吸收被确定为自我乳化制剂的关键途径.
结论:
- CTX S-SEDDS有效地提高了cabazitaxel的口服生物可用性.
- 开发的系统克服了与传统SEDDS相关的局限性.
- CTX S-SEDDS提供了一个有前途的固体剂型,具有固体和液体制剂的双重优势.
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