The influence of Pluronics L64, F68, F88 and F127 on the solubility and membrane permeability of leflunomide (LEF) in acidic and alkaline buffer solutions with physiological pHs was revealed. A noticeable increase of LEF solubility in the presence of Pluronics was revealed. It was demonstrated that the structure of Pluronics has influence on the manifestation of a solubilizing effect. Namely, more efficient solubilizers for LEF were found to be L64 and F127, having the lowest content of ethylene oxide groups in the structure and lower HLB indices in comparison with F68 and F88. The binding of LEF with the core of Pluronic micelles was proposed on the basis of the obtained ¹Н NMR data. Permeability of LEF through an artificial Permeapad barrier composed of phospholipids was measured using the Franz diffusion cell. Decrease of the LEF permeability in the presence of all investigated Pluronics was detected. The location of hydrophobic fragment of LEF molecule inside the micelle leads to a decrease in the non-polar surface area and the ability of the drug to pass through the lipophilic layer of the membrane.

揭示了Pluronics L64，F68，F88和F127对来氟米特（LEF）在具有生理pH的酸性和碱性缓冲溶液中的溶解度和膜通透性的影响。揭示了在Pluronics存在下LEF溶解度的显着增加。已证明，Pluronics的结构对增溶作用的表现有影响。即，发现LEF的更有效的增溶剂是L64和F127，与F68和F88相比，其结构中的环氧乙烷基团含量最低并且HLB指数较低。在获得的¹的基础上，提出了LEF与Pluronic胶束核心的结合。核磁共振数据。使用Franz扩散池测量LEF通过由磷脂组成的人工Permeapad屏障的渗透性。在所有研究过的Pluronics存在下，LEF通透性降低。LEF分子的疏水片段在胶束内部的位置会导致非极性表面积的减少以及药物穿过膜亲脂层的能力降低。