帕克利塔塞尔从聚合物微粒中快速in vivo释放
Haisheng He1, Jianping Qi1, Yi Lu1,2,3
1School of Pharmaceutical Sciences, Fudan University, Key Laboratory of Smart Drug Delivery of MOE and National Key Laboratory of Advanced Drug Formulations for Overcoming Delivery Barriers, Shanghai 201203, China.
药物纳米载体释放在聚合物微粒 (PMs) 中使用帕克利塔塞尔 (PTX) 进行了研究. 结果显示PTX在体内迅速释放,这表明PM作为溶解剂,而不是向的输送载体.
科学领域:
- 纳米医学是一种纳米医学.
- 药理动力学 药理动力学
- 聚合物化学 聚合物化学
背景情况:
- 准确的纳米载体体体内药物释放概况对于临床转化至关重要.
- 目前的方法缺乏释放或残留药物的直接量化.
- 聚合物微粒 (PMs) 正在研究药物输送应用.
研究的目的:
- 估计来自mPEG-PDLLA聚合菌粒 (PMs) 的帕克利塔塞尔 (PTX) 在体内释放动力学.
- 开发一种间接方法来评估纳米载体释放的药物.
主要方法:
- 血液药理动力学 (PTX量化) 与粒子动力学 (近红外标记的PMs) 的比较.
- 监测PTX与共聚合物比率的动态变化.
- 使用聚合引起的灭光体用于粒子跟踪.
主要成果:
- 在体内证明了PMs中PTX的惊人快速释放.
- 超过88.2%的PTX在服用后15秒内释放出来.
- 大约99.0%的PTX在服药5分钟后释放出来.
结论:
- 在体内,PTX从mPEG-PDLLA聚合菌根中快速释放.
- PMs可能主要作为PTX的溶解剂起作用.
- 这些发现挑战了这些PM作为有针对性的交付工具的作用.
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