Quantifying Drug Cargo Partitioning in Block Copolymer Micelle Solutions,ACS Applied Polymer Materials

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Quantifying Drug Cargo Partitioning in Block Copolymer Micelle Solutions
ACS Applied Polymer Materials ( IF 4.4 ) Pub Date : 2020-08-24 , DOI: 10.1021/acsapm.0c00694
Xiuli Li ₁ , Veera Venkata Shravan Uppala ₁ , Tyler J. Cooksey ₂ , Megan L. Robertson ₂ , Louis A. Madsen ₁

Affiliation

Understanding molecular partitioning in solution is crucial for the design of micelle-based formulations. We investigate PEO–PPO–PEO triblock copolymer micelles and their solubilization of three hydrophobic drugs: hydrochlorothiazide, indomethacin, and paclitaxel. Using NMR diffusometry, we quantify the diffusion coefficients of different species in solution, including polymers, drug cargo molecules, and solvent molecules. Polymer concentration and drug chemistry changes cause effects such as increasing partition percentages of hydrochlorothiazide and indomethacin within micelles as the F127 concentration increases from 1 to 5% w/v. This facile methodology enables quantification of drug distribution in micelles without perturbation of the solution, thus opening opportunities to understand broader processes of cargo partitioning.

中文翻译：

定量嵌段共聚物胶束溶液中的药物分配

了解溶液中的分子分配对于基于胶束的配方设计至关重要。我们研究了PEO–PPO–PEO三嵌段共聚物胶束及其对三种疏水性药物的溶解：氢氯噻嗪，消炎痛和紫杉醇。使用核磁共振扩散法，我们可以量化溶液中不同物质的扩散系数，包括聚合物，药物货物分子和溶剂分子。聚合物浓度和药物化学变化会引起影响，例如随着F127浓度从1增加到5％w / v，氢氯噻嗪和消炎痛在胶束中的分配百分比增加。这种简便的方法可以在不干扰溶液的情况下对胶束中的药物分布进行定量，从而为了解更广泛的货物分配过程提供了机会。

更新日期：2020-09-11

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