多功能灵活的囊,整合粘膜透和肠道向,有效地进行巴克利塔克塞尔口服
Chao Liu1,2, Wei Liu1,3, Yanhong Liu1,2
1State Key Laboratory of Bioactive Substance and Function of Natural Medicines, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China.
Acta pharmaceutica Sinica. B
|September 1, 2023
概括
这项研究开发了新型菌株 (PTX@GNPs),以克服口服帕克利塔塞尔 (PTX) 的生物可用性挑战. 这些菌根增强了药物输送,显示了与注射相比的抗瘤疗效,并提高了口服化疗的有效性.
科学领域:
- 生物医学工程 生物医学工程
- 药物输送系统 药物输送系统
- 纳米技术纳米技术
背景情况:
- 口服帕克利塔塞尔 (PTX) 由于胃肠道障碍,具有较差的生物利用性.
- 克服肠道物理化学障碍需要先进的药物输送系统.
研究的目的:
- 构建一种新型的菌根系统 (PTX@GNPs),以增强口服帕克利塔塞尔的输送.
- 应对包括粘液阻塞和上皮壁垒在内的挑战.
主要方法:
- 合成了一种新型聚合物 (Fmoc-PEG-GCA) 来制造高密度PEGylated,用甘油酸装饰的小粒.
- 使用Fmoc进行PTX封装,通过ππ堆叠和PEG实现灵活性.
- 通过使用甘醇酸 (GCA) 成分研究粘液逃逸和上皮向.
主要成果:
- PTX@GNPs证明了粘液捕获逃脱和增强肠道上皮的向.
- 在体外和体内研究证实了PTX的口服生物可用性得到改善.
- 口服PTX@GNPs的抗瘤疗效与静脉注射Taxol相比较.
结论:
- 开发的PTX@GNP有效地提高了口服帕克利塔塞尔的生物可用性和抗瘤功效.
- 该系统通过增加体内药物保留时间和重塑免疫微环境,为改善口服化疗提供了潜力.
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