We investigated the effect of fatty acid chain length on the binding capacity of drug and fatty acid to Pluronic F127-based microemulsions. This was accomplished by using turbidity experiments. Pluronic-based oil-in-water microemulsions of various compositions were synthesized and titrated to turbidity with concentrated Amitriptyline, an antidepressant drug. Sodium salts of C(8), C(10), or C(12) fatty acid were used in preparation of the microemulsion and the corresponding binding capacities were observed. It has been previously determined that, for microemulsions prepared with sodium caprylate (C(8) fatty acid soap), a maximum of 11 fatty acid molecules bind to the microemulsion per 1 molecule of Pluronic F127 and a maximum of 12 molecules of Amitriptyline bind per molecule of F127. We have found that with increasing the chain length of the fatty acid salt component of the microemulsion, the binding capacity of both the fatty acid and the Amitriptyline to the microemulsion decreases. For sodium salts of C(8), C(10) and C(12) fatty acids, respectively, a maximum of approximately 11, 8.4 and 8.3 molecules of fatty acid molecules bind to 1 Pluronic F127 molecule. We propose that this is due to the decreasing number of free monomers with increasing chain length. As chain length increases, the critical micelle concentration (cmc) decreases, thus leading to fewer monomers. Pluronics are symmetric tri-block copolymers consisting of propylene oxide (PO) and ethylene oxide (EO). The polypropylene oxide block, PPO is sandwiched between two polyethylene oxide (PEO) blocks. The PEO blocks are hydrophilic while PPO is hydrophobic portion in the Pluronic molecule. Due to this structure, we propose that the fatty acid molecules that are in monomeric form most effectively diffuse between the PEO "tails" and bind to the hydrophobic PPO groups.

译文

我们研究了脂肪酸链长度对药物和脂肪酸与Pluronic F127-based微乳液结合能力的影响。这是通过使用浊度实验完成的。合成了各种组成的基于Pluronic的水包油微乳液,并用浓缩的阿米替林 (一种抗抑郁药) 滴定至浊度。在微乳液的制备中使用C(8),C(10) 或C(12) 脂肪酸的钠盐,并观察到相应的结合能力。先前已经确定,对于用辛酸钠 (C(8) 脂肪酸皂) 制备的微乳液,每1分子Pluronic F127最多有11个脂肪酸分子与微乳液结合,每分子F127最多有12个阿米替林结合。我们发现,随着微乳中脂肪酸盐成分的链长增加,脂肪酸和阿米替林与微乳的结合能力均降低。对于C(8) 、C(10) 和C(12) 脂肪酸的钠盐,最多约11、8.4和8.3分子的脂肪酸分子与1个Pluronic F127分子结合。我们认为这是由于随着链长的增加,自由单体的数量减少所致。随着链长的增加,临界胶束浓度 (cmc) 降低,从而导致单体减少。Pluronics是由环氧丙烷 (PO) 和环氧乙烷 (EO) 组成的对称三嵌段共聚物。聚丙烯氧化物块PPO夹在两个聚环氧乙烷 (PEO) 块之间。PEO嵌段是亲水的,而PPO是Pluronic分子中的疏水部分。由于这种结构,我们建议单体形式的脂肪酸分子最有效地在PEO “尾巴” 之间扩散并与疏水性PPO基团结合。

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