通过设计指导的质量开发隐蔽的Everolimus脂肪体配方:系统的优化和评估
Simranjeet Kaur1, Rajveer Singh2, Dilpreet Singh1
1Department of Pharmaceutics, ISF College of Pharmacy, GT Road, Moga 142001, Punjab, India.
Current drug metabolism
|September 10, 2024
概括
这项研究开发了一种新型隐形脂质体配方 (S-EVE-LIPO) 用于Everelimus (EVE),以提高生物可用性和减少副作用. 在临床前研究中,增强的配方证明了持续的药物释放和改善的治疗疗效.
科学领域:
- 纳米医学是一种纳米医学.
- 药物输送系统 药物输送系统
- 癌症治疗方法 癌症治疗方法
背景情况:
- 埃弗罗利斯 (EVE) 用于HR+晚期乳腺癌,但其口服生物可用性较低,并具有严重的皮肤副作用.
- 口服EVE导致皮疹,唇部和口腔.
- 需要改善药物输送,以提高疗效和患者的遵守性.
研究的目的:
- 为了提高everolimus的生物可用性和治疗疗效.
- 开发一种隐蔽的脂肪体配方 (S-EVE-LIPO),用于静脉注射.
- 为了减轻与口服everolimus相关的副作用.
主要方法:
- 脂质体是使用薄膜水化方法来制备的.
- 脂质体表面被维生素E TPGS (多科菲尔聚乙烯甘醇糖酸盐) 修改.
- 使用D-最佳混合物设计优化了配方,并分析了尺寸,封装和释放动力学.
主要成果:
- 优化的S-EVE-LIPO表现出纳米尺寸 (99.5 ± 3.70 nm) 和高封装效率 (81.5 ± 2.86%).
- 与非隐形脂肪体相比,S-EVE-LIPO显示了持续的药物释放 (48小时内90.22%)
- 在体外研究表明,IC50较低,细胞吸收增加,ROS生成,以及与维生素ETPGS的血红相容性改善.
结论:
- 维生素ETPGS是提高脂质体常利蒙药疗效的关键添加剂.
- 该S-EVE-LIPO配方提供了降低毒性和剂量频率的潜力.
- 这种新的配方显示出改善乳腺癌治疗的希望.
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