离子复合物作为在水中的药物溶解剂
Frank Boateng Osei1, Kwaku Twum1, Barbara Manfredi2
1Oakland University, Department of Chemistry 146 Library Drive Rochester MI 48309-4479 USA beyeh@oakland.edu.
RSC advances
|October 29, 2024
概括
水友性复合素显著提高了疏水性药物的水溶性,如异化,咖啡因和灰色. 这些resorcinarene-药物复合体没有表现出细胞毒性,表明它们有可能作为药物输送辅助剂.
科学领域:
- 超分子化学 超分子化学
- 材料科学 材料科学 材料科学
- 制药科学 制药科学
背景情况:
- 众所周知,Resorcinarenes具有宿主-客人复杂性,但在制药应用中未得到充分探索.
- 提高疏水性药物的水溶性对于有效的药物输送至关重要.
研究的目的:
- 调查水友性复合素作为防水药物溶解剂的潜力.
- 评估Resorcinarenes对异化,咖啡因和灰色的水溶性和输送的影响.
主要方法:
- 动态光散射 (DLS) 用于评估粒子大小变化.
- 异热定位热量计 (ITC) 用于量化结合亲缘关系.
- 核磁共振 (NMR) 光谱 (1H NMR) 用于确认分子相互作用.
主要成果:
- 与纯药物溶液相比,resorcinarene与药物混合物表现出更好的溶解度和清晰度.
- DLS显示了药物颗粒大小的转移到resorcinarene宿主范围.
- 1H NMR证实了与化学转移变化的相互作用,从-0.20到0.81 ppm.
- ITC显示了0.54和211mM之间的结合亲和力.
- 对HEK-293细胞的细胞毒性研究表明,在200μM以下没有任何不良影响.
结论:
- 水友性复合素有效地提高了疏水性药物的水溶性.
- 树脂烯药物复合体显示出有利的结合相互作用,缺乏细胞毒性.
- 树脂烯宏循环显示出作为新型药物溶解剂的承诺,用于制药应用.
相关概念视频
Factors Affecting Dissolution: Particle Size and Effective Surface Area
745
Dissolution kinetics, an essential aspect of oral drug delivery, is significantly influenced by the drug's particle size. According to the Noyes-Whitney dissolution model, the dissolution rate correlates directly with the drug's surface area. The larger the surface area, the higher the drug's solubility in water, leading to a faster drug dissolution rate. Reducing particle size increases the effective surface area, enhancing the dissolution process. Micronization and nanosizing are...
745
Phase I Reactions: Reductive Reactions
181
Phase I biotransformation reductive reactions are chemical processes that modify drugs by introducing or revealing polar functional groups via reduction. Enzymes called reductases catalyze these reactions, playing a pivotal role in drug metabolism by transforming lipophilic drugs into more polar, water-soluble metabolites for easy excretion. An essential type of reductive reaction is the carbonyl group reduction, where aldehydes and ketones are reduced to alcohols. An example is the...
181
Racemic Mixtures and the Resolution of Enantiomers
18.1K
A racemic mixture, or racemate, is an equimolar mixture of enantiomers of a molecule that can be separated using their unique interaction with chiral molecules or media. Racemic mixtures are denoted by the (±)- prefix. This ‘optical rotation descriptor’ applies to the whole solution of a racemic mixture rather than a specific stereoisomer. Enantiomers typically have the same physical and chemical properties. Hence, they are not easily separable. However, enantiomers can exhibit...
18.1K
Recrystallization: Solid–Solution Equilibria
1.0K
Recrystallization is a purification technique used to separate impurities from solid compounds. In this technique, no chemical reactions occur. Instead, it exploits physical properties only, specifically, the solubility differences between the desired compound and impurities, either at a single temperature or at different temperatures, and under other selected conditions. The solid-solution equilibrium (solubility equilibrium) of each component in the solution represents a binary phase...
1.0K
Factors Influencing Drug Absorption: Drug Dissolution
423
The pharmacokinetic journey of drugs from solid oral dosage forms into systemic circulation is multifaceted. It begins with disintegration, a prerequisite ensuring a solid dosage form's subdivision into minute particles. Dissolution occurs next as these granulated entities solubilize in gastrointestinal fluids. This solubilization is crucial for the succeeding stage, permeation, which describes the traversal of the drug across the intestinal membrane and its subsequent entry into the blood...
423
Drug-Receptor Bonds
2.7K
Drug-receptor bonds are formed through various chemical forces when drugs interact with target cells. Covalent bonds, strong and irreversible, are exemplified by DNA-alkylating anticancer agents that inhibit cell division. However, such irreversible drug binding lacks selectivity and can modify the DNA of the surrounding healthy cells. Covalent binding often contributes to tissue toxicity, as seen with chloroform and paracetamol metabolites binding to the liver, causing hepatotoxicity.
In...
In...
2.7K


