关于提高口服生物可用性的大麻素载荷溶解系统的比较研究:基于脂质体和环氧素的配方
Hideyuki Sato1, Kenta Watanabe1, Ryuji Yagi2
1Laboratory of Biopharmacy, School of Pharmaceutical Sciences, University of Shizuoka, Shizuoka, Japan.
Biopharmaceutics & drug disposition
|December 27, 2025
概括
与晶体CBD相比,开发脂质体大麻 (LIP/CBD) 显著提高了其溶解和口服生物可用性 (BA). 这种脂质体配方为改善CBD提供了一个有希望的策略.
科学领域:
- 药理学和制药学 药理学和制药学
- 药物输送系统 药物输送系统
- 基于脂质的配方 脂质的配方
背景情况:
- 大麻二醇 (CBD) 呈现出不良的物理化学特性,包括低溶解度和分散性,限制了其口服生物利用性.
- 第一通代谢进一步降低了口服CBD的全身暴露.
- 传统的溶化系统,如基于环氧素 (CD/CBD) 的配方,提供了一些改善,但可能无法完全解决CBD的局限性.
研究的目的:
- 开发一种脂质体内大麻 (LIP/CBD) 配方,以增强CBD的物理化学特性和口服生物可用性 (BA).
- 为了比较LIP/CBD与晶体CBD和常规循环烯基配方 (CD/CBD) 的生物制药性能.
主要方法:
- 使用溶剂注射方法制备了脂质体大麻二醇 (LIP/CBD).
- 物理化学表征包括粒子大小,泽塔潜力和在模拟的肠道pH下溶解的研究.
- 药物动力学评估涉及体内口服,以评估全身暴露和Tmax.
主要成果:
- LIP/CBD表现出均的球形脂质体 (~120 nm,PDI 0.13,泽塔电位 -68 mV).
- 与晶体CBD相比,LIP/CBD显示CBD溶解率增加了8倍.
- 口服LIP/CBD导致系统暴露量比晶体CBD高22倍,显著超过CD/CBD (5.3倍增加).
结论:
- 脂质体封装是一种可行的策略,可以克服CBD的溶解性差,并增强其溶解和口服吸收.
- LIP/CBD比晶体CBD和常规环氧素配方具有优越的生物制药优势.
- 脂质成分可能导致的淋巴吸收增强可能解释了LIP/CBD的延长Tmax.
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