硫酸的发展和生物活性 甲酸的交叉链接多糖化物输送系统
Natallia V Dubashynskaya1, Anton N Bokatyi1, Andrey S Trulioff2
1Institute of Macromolecular Compounds of the Russian Academy of Sciences, Bolshoi VO 31, 199004 Saint Petersburg, Russia.
Pharmaceutics
|October 28, 2023
概括
研究人员开发了一种新型的甲酸 (DexP) 输送系统,使用了氨酸和奇托桑. 这种系统增强了药物的生物可用性,降低了毒性,保持了抗炎疗效.
科学领域:
- 生物制药药物药物输送
- 聚合物科学 聚合物科学
- 纳米技术 纳米技术
背景情况:
- 改善葡萄糖皮质类生物制药性质,例如增加局部生物可用性和减少全身毒性,仍然是一个重大挑战.
- 德克萨米他酸盐 (DexP) 是一种广泛使用的葡萄糖皮质类药物,具有局部递送的潜力,以提高疗效并最大限度地减少副作用.
研究的目的:
- 开发一种新型的甲酸 (DexP) 输送系统,利用氨酸 (HA) 和一种水溶性酸衍生物,二甲基氨基乙基酸 (DEAECS).
- 描述开发的DexP输送系统的物理化学特性,药物加载,释放动力学和粘粘性特性.
主要方法:
- 在酸 (HA) 和二甲基氨基乙基基 (DEAECS) 之间形成一个多电解质复合物 (PEC),离子作为交联剂.
- PECs的表征,包括水力动力直径, ζ-潜力,封装效率和DexP含量.
- 评估DexP载荷PECs的粘膜粘合,药物释放概况和体外抗炎活性.
主要成果:
- 开发的DexP输送系统形成了PEC,其水力动力直径为244nm, ζ电位为+24.4mV.
- 获得了高封装效率 (75.6%) 和DexP含量 (45.4μg/mg).
- 这些系统表现出了出色的粘膜粘附性和延长药物释放 (大约2个小时). 在10小时内释放70%),同时保持DexP的抗炎活性.
结论:
- 开发的HA-DEAECS-Zn多电解质复合物是一种有前途的纳米载体,用于甲酸的输送.
- 该系统通过增强粘膜粘合和控制药物释放,有效地改善生物制药性质.
- 该配方保留了甲酸的治疗性抗炎活性,这表明有可能减少全身毒性和改善局部疗效.
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