用生物相容合成脂质制备的黄素载体固体脂质纳米颗粒的物理化学表征,稳定性和体外评估
Swagata Patra1, Joykrishna Dey1, Avik Chakraborty2
1Department of Chemistry, Indian Institute of Technology Kharagpur, Kharagpur 721302, India.
ACS applied bio materials
|July 5, 2023
概括
新的氨基酸衍生脂质改善固体脂质纳米颗粒 (SLN) 以提高黄素的输送. 这些稳定的SLN显示了药物捕获和释放的改善,为难溶性药物提供了有前途的纳米载体.
科学领域:
- 纳米技术 纳米技术
- 材料科学 材料科学 材料科学
- 药理学 药理学是指药理学的学科.
背景情况:
- 固体脂质纳米颗粒 (SLN) 是先进的药物递送系统,特别是对于水溶性较差的化合物.
- 对SLN的挑战包括水稳定性,受控的药物释放和生物相容性.
- 开发新的脂质对于优化SLN性能至关重要.
研究的目的:
- 开发新的氨基酸衍生脂质,用于增强黄素载荷的SLN.
- 研究脂质头组极性对SLN稳定性和特征的影响.
- 评估从优化的SLN中黄素的捕获效率,稳定性和体外释放.
主要方法:
- 合成两种氨基酸衍生脂质,具有不同的头组极性.
- 用库尔库载入的SLN的制备和表征 (形态,颗粒大小,捕获效率).
- 评估水性稳定性,储存稳定性和体外药物释放动力学.
- 使用PC3和MCF7细胞系进行细胞毒性评估.
主要成果:
- 优化的SLN配方实现了高黄素捕获效率,超过了文献价值.
- SLN分散体表现出改善的水性和储存稳定性,受脂质头组极性的影响.
- 载有黄素的SLN在体外表现出更高的药物释放率,特别是那些含有-OH组的SLN.
- 黄素及其SLN配方显示出对PC3和MCF7细胞的度依赖性细胞毒性.
结论:
- 新型半合成脂质可以形成稳定的固体脂质纳米颗粒悬浮物,以有效提供黄素.
- 脂质头组的极性显著影响SLN稳定性和药物释放概况.
- 这些优化的SLN代表了提供水溶性较差的药物 (如黄素) 的有希望的平台.
相关概念视频
01:20Factors Affecting Dissolution: Drug Permeability, Stability and Stereochemistry
231
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...
231
01:22Factors Influencing Drug Absorption: Physicochemical Parameters
330
The physicochemical characteristics of drugs play a crucial role in formulating stable and bioavailable drug products. The solubility of a drug, governed by the varying pH along the GI tract and its dissociation constant (pKa), is pivotal in determining its ionization state and absorption rate. Notably, weak acids and bases remain unionized and are absorbed more rapidly.
Enhanced drug absorption can be achieved by reducing particle sizes and increasing surface areas, thereby facilitating...
Enhanced drug absorption can be achieved by reducing particle sizes and increasing surface areas, thereby facilitating...
330
01:21Factors Affecting Dissolution: Drug pKa, Lipophilicity and GI pH
1.6K
Drug absorption within the gastrointestinal (GI) tract is a complex process influenced by several critical factors, including the site pH, the drug's dissociation constant (pKa), and the drug's lipophilicity. The GI tract exhibits a pH gradient, with an acidic environment in the stomach and a more alkaline environment in the small intestine. This pH variation directly affects the ionization state of drugs.
A drug's pKa and the pH of the gastrointestinal (GI) tract play crucial roles...
A drug's pKa and the pH of the gastrointestinal (GI) tract play crucial roles...
1.6K