芳香化脂质体用于持续的药物输送
Yang Li1, Tianjiao Ji1, Matthew Torre2
1Laboratory for Biomaterials and Drug Delivery, Department of Anesthesiology, Division of Critical Care Medicine, Children's Hospital Boston, Harvard Medical School, Boston, MA, 02115, US.
Nature communications
|October 20, 2023
概括
芳香性脂质体增强药物负载并减少泄漏,延长治疗时间并降低毒性. 这种新的方法改善了对各种有效载荷的脂质体药物递送,包括难以封装的分子,如四毒素.
科学领域:
- 生物材料科学 生物材料科学
- 纳米技术纳米技术
- 制药科学 制药科学
背景情况:
- 脂质体药物递送系统面临的挑战是药物负载不足和有效载荷泄漏,限制有效性和增加毒性.
- 这些问题影响了脂质体配方的作用持续时间和安全性.
研究的目的:
- 通过开发具有改善药物加载和受控释放的芳香化脂质体来解决脂质体药物递送的局限性.
- 研究将芳香基纳入脂质双层对有效载荷封装和释放动态的影响.
主要方法:
- 合成脂与共结合的芳香基被用于创建芳香化脂质体.
- 评估了各种有效载荷 (小分子,宏分子) 的封装效率和释放概况.
- 装有四毒素的芳香性脂质体在局部麻醉模型中进行了测试.
主要成果:
- 芳香化脂质体表现出药物载荷能力增加,用于广泛的有效载荷.
- 与传统的脂质体相比,观察到明显减少的突发释放和延长的释放时间.
- 含有四毒素的芳香化脂质体表现出长时间的麻醉作用和体内毒性降低.
结论:
- 脂质双层的芳香化是一种可行的策略,可以提高脂质体药物递送系统的性能.
- 这种修改改善了药物封装,控制了释放率,并为更安全,更有效的疗法提供了潜力.
- 芳香性脂质体代表了临床应用的有希望的进步,特别是对于具有挑战性的有效载荷.
相关概念视频
Factors Affecting Dissolution: Drug Permeability, Stability and Stereochemistry
209
Orally administered drugs primarily enter the systemic circulation via passive diffusion through the intestinal membranes. The drug's absorption is influenced by drug stability in the gastrointestinal GI tract, membrane permeability, the surface area available for absorption, luminal drug concentration, and residence time in the lumen. Drug permeability can be enhanced by adjusting the lipophilicity, polarity, or molecular size of the drug, promoting its passive transport across intestinal...
209
Drug Delivery: Overview
300
The selection of a drug's delivery route depends upon its physicochemical properties, including lipid or water solubility and ionization, as well as the therapeutic requirement, such as immediate or sustained effect. These routes can be divided into three primary categories: enteral, parenteral, and topical.
Enteral delivery involves administering drugs directly through swallowing, sublingual placement, or buccal application. Orally administered drugs predominantly navigate the...
Enteral delivery involves administering drugs directly through swallowing, sublingual placement, or buccal application. Orally administered drugs predominantly navigate the...
300
Lipid Absorption
495
Dietary triglycerides from chyme in the duodenum are mixed with bile salts produced by the liver to emulsify fats. As a result, large droplets are broken down into smaller ones, increasing the surface area for enzymatic action. Once emulsified, pancreatic lipases hydrolyze the triglycerides into free fatty acids and monoglycerides.
These breakdown products bind with bile salts and lecithin to form micelles, which quickly pass between microvilli to come in close contact with the apical...
These breakdown products bind with bile salts and lecithin to form micelles, which quickly pass between microvilli to come in close contact with the apical...
495


