甘醇,薄荷醇:薄荷醇深溶剂及其混合物对角层成分的结构和分子流动性的影响
Grzegorz S Czyrski1, Runtian Qie2, Emma Sparr2
1LEO Foundation Center for Cutaneous Drug Delivery, Department of Pharmacy, University of Copenhagen, 2100 Copenhagen, Denmark.
International journal of pharmaceutics
|May 14, 2025
概括
烯基醇 (PG) 和薄荷醇: 硫醇深度溶解剂 (DES) 混合物增强了克洛特里马的皮肤透. PG影响角细胞,而DES影响脂质矩阵,导致药物和PG通道增加.
科学领域:
- 制药科学 制药科学
- 材料科学 材料科学 材料科学
- 生物物理学的生物物理.
背景情况:
- 角层 (SC) 是通过皮肤传递药物的主要障碍.
- 了解透增强剂如何与SC脂质和蛋白质相互作用,对于优化药物透至关重要.
研究的目的:
- 为了研究烯基醇 (PG),薄荷:硫醇深溶解剂 (DES) 和它们的混合物对SC结构和组成的影响.
- 阐明这些配方调节克洛特里马透的机制.
主要方法:
- 猪SC暴露于PG,DES和PG:DES与不同的PG度混合.
- 使用FTIR光谱学分析SC脂质提取,脂质排列和角质二次结构.
- 通过13C MAS NMR光谱对SC脂质和蛋白质分子运动的评估.
主要成果:
- PG:DES混合物 (10-50%的PG) 提取的SC脂比纯的DES更多;纯的PG提取的较少.
- 配方稍微松动了SC脂质包装,并促进了质蛋白的α-螺旋转向β-片的过渡.
- DES显著增加了SC脂质和蛋白质的流动性;PG的影响很小. 混合物的效果取决于DES含量.
结论:
- 在PG:DES混合物中,克洛特里马的增强透性归因于PG对角细胞的作用和DES对SC脂质基质的影响.
- PG促进细胞内药物透,而DES通过改变包装和移动性来增强通过细胞间脂质的通道.
- 结合PG和DES提供了一种协同方法,以改善通过皮肤递送药物.
相关概念视频
02:17Physical Properties of Ethers
6.8K
Overview
An ether molecule has a net dipole moment due to the polarity of C–O bonds. Subsequently, boiling points of ethers are lower than those of alcohols of comparable molecular weight and slightly higher than those of hydrocarbons of comparable molecular weight (Table 1).
Ethers can act as hydrogen bond acceptors, making them more water-soluble than hydrocarbons, but since ethers cannot act as hydrogen bond donors, they are much less soluble in water than alcohols. Ethers are...
An ether molecule has a net dipole moment due to the polarity of C–O bonds. Subsequently, boiling points of ethers are lower than those of alcohols of comparable molecular weight and slightly higher than those of hydrocarbons of comparable molecular weight (Table 1).
Ethers can act as hydrogen bond acceptors, making them more water-soluble than hydrocarbons, but since ethers cannot act as hydrogen bond donors, they are much less soluble in water than alcohols. Ethers are...
6.8K
02:32Physical Properties of Alcohols and Phenols
13.8K
Alcohols are organic compounds in which a hydroxy group is attached to a saturated carbon. Phenols are a class of alcohols containing a hydroxy group attached to an aromatic ring. The physical properties of the alcohols and phenols are influenced by hydrogen bonding due to the oxygen–hydrogen dipole in the hydroxy functional group and dispersion forces between alkyl or aryl regions of alcohol and phenol molecules.
Alcohols possess a higher boiling point than aliphatic hydrocarbons of...
Alcohols possess a higher boiling point than aliphatic hydrocarbons of...
13.8K
02:34Comparing Intermolecular Forces: Melting Point, Boiling Point, and Miscibility
43.5K
Intermolecular forces are attractive forces that exist between molecules. They dictate several bulk properties, such as melting points, boiling points, and solubilities (miscibilities) of substances. Molar mass, molecular shape, and polarity affect the strength of different intermolecular forces, which influence the magnitude of physical properties across a family of molecules.
Temporary attractive forces like dispersion are present in all molecules, whether they are polar or nonpolar. They...
Temporary attractive forces like dispersion are present in all molecules, whether they are polar or nonpolar. They...
43.5K
03:22Colloids
17.2K
Children at play often make suspensions such as mixtures of mud and water, flour and water, or a suspension of solid pigments in water known as tempera paint. These suspensions are heterogeneous mixtures composed of relatively large particles that are visible to the naked eye or can be seen with a magnifying glass. They are cloudy, and the suspended particles settle out after mixing. On the other hand, a solution is a homogeneous mixture in which no settling occurs and in which the dissolved...
17.2K
01:20Factors Affecting Dissolution: Drug Permeability, Stability and Stereochemistry
158
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...
158
02:12Solvating Effects
7.2K
An understanding of the solvating effect helps rationalize the relation between solvation and acidity of the compound. In addition, this also explains the relative stability of conjugate bases for compounds with different pKa values. This lesson details, in-depth, the principle of solvating effects. The strength of an acid and the stability of its corresponding conjugate base are determined using pKa values. This observed relationship is a consequence of solvation, which is the interaction...
7.2K