在α-Tocopherol和DMSO溶液中缩的Cabazitaxel的局部药物输送
Boyang Sun1, Georgios Paraskevopoulos2, Jiwei Min1
1School of Chemical Engineering and Technology, Key Laboratory of Systems Bioengineering (Ministry of Education), Frontiers Science Center for Synthetic Biology (Ministry of Education), State Key Laboratory of Chemical Engineering, Tianjin University, Tianjin, 300350, P. R. China.
Advanced science (Weinheim, Baden-Wurttemberg, Germany)
|August 9, 2023
概括
在新型溶剂中的局部卡巴西 (CTX) 增强了皮肤透,并在临床前模型中抑制了皮肤癌的生长. 这种配方在治疗皮肤恶性瘤方面表现有前途.
科学领域:
- 皮肤病学 皮肤病学
- 在瘤学瘤学.
- 药品制造 药品制造 药品制造
背景情况:
- 局部化疗对于治疗特定的皮肤癌症至关重要.
- 卡巴西塔塞尔 (CTX) 是一种强大的细胞毒剂.
- 开发有效的局部药物输送系统对于改善治疗结果至关重要.
研究的目的:
- 为了研究cabazitaxel (CTX) 在α-托科菲醇和二甲基硫氧化物 (DMSO) 混合物中的溶解性和皮肤透性.
- 在临床前皮肤癌模型中评估局部CTX配方的抗瘤疗效.
主要方法:
- 在α-托科菲罗尔中高度溶解CTX.
- 核磁共振 (NMR) 和分子动力学 (MD) 用于配方分析.
- 在体外人体皮肤透性研究和跨皮肤水分损失测定.
- 在裸体小鼠中进行体内抗瘤疗效测试,这些小鼠患有异种植皮肤癌.
主要成果:
- 在高度 (>100毫克/毫升) 的情况下,CTX会溶解在α-托科菲罗尔中.
- 添加30%的DMSO在体外显著提高CTX皮肤透率 (24小时内≥5μg/cm2).
- DMSO/α-托科菲罗尔配方显示可逆性皮肤屏障效应和显著的瘤生长抑制 in vivo.
结论:
- 与DMSO和α-托科菲罗尔配制的局部卡巴西塔塞尔 (CTX) 显示了增强的皮肤透和强大的抗瘤活性.
- 这种新的局部输送系统需要进一步研究治疗皮肤恶性瘤.
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