提莫金载脂质纳米囊分散:用于口服的两种制备方法,表征和体外评估
Mouna Selmi1, Amine Trabelsi1,2, Nolwenn Lautram3
1Laboratoire des substances naturelles bioactives et biotechnologie LR24ES14, Faculté de médecine dentaire, Université de Monastir, Tunisia.
Pharmaceutical development and technology
|January 3, 2025
概括
研究了两种方法,用于将Thymoquinone (TQ) 封装成脂质纳米囊 (LNC),用于口服. 这两种方法都产生了稳定的LNCs,在模拟的胃肠液中药物释放有限,显示了TQ口服的潜力.
科学领域:
- 纳米技术纳米技术
- 制药科学 制药科学
- 药物运输 药物运输 药物运输
背景情况:
- 蒂莫金 (TQ) 具有治疗潜力,但由于生物可用性差,在口服时面临挑战.
- 脂质纳米囊 (LNCs) 提供了一种有前途的策略,用于封装像TQ这样的疏水药物,增强它们的输送.
- 开发有效的口服配方对于最大限度地提高TQ的治疗效益至关重要.
研究的目的:
- 调查两种不同的方法来封装Thymoquinone (TQ) 进入脂质纳米囊 (LNC).
- 评估TQ装载的LNCs的物理化学性质,稳定性和肠道透性,用于口服.
- 评估LNCs作为Thymoquinone可行的口服输送系统的适用性.
主要方法:
- 采用了两种封装技术:在相位逆转温度 (PIT) 方法 (TQ-LNCs-1) 中加入TQ,并将TQ添加到预制的LNCs分散 (TQ-LNCs-2).
- 特性包括纳米粒子大小,多分散性指数 (PDI),泽塔潜力,药物负载 (DL) 和存储稳定性.
- 试验室评估涉及模拟胃肠液 (SGIF) 的稳定性和使用Caco-2细胞单层的肠透性研究.
主要成果:
- 无论是TQ-LNCs-1还是TQ-LNCs-2,都产生了平均直径约为58-61nm和可接受的PDI值的纳米粒子.
- 获得的药物负载为TQ-LNCs-1的8.7 ± 0.2 mg/mL和TQ-LNCs-2的7.7 ± 0.6 mg/mL.
- 在SGIF中观察到的TQ释放率不到14%,而LNC配方与自由TQ相比,肠道透率略有增加.
结论:
- 脂质纳米囊 (LNCs) 提供了一个有前途的配方,用于口服Thymoquinone (TQ).
- 将TQ添加到现有的LNC分散的方法是一种可行的方法,可以扩展到其他药物.
- 装有TQ的LNC显示出良好的稳定性,并有可能改善thymoquinone的口服生物可用性.
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