Mazur Aleksy, Neugebauer Dorota
Department of Physical Chemistry and Technology of Polymers, Faculty of Chemistry, Silesian University of Technology, 44-100 Gliwice, Poland.
Pharmaceutics. 2023 Oct 30;15(11):2556. doi: 10.3390/pharmaceutics15112556.
An ionic liquid based on the monomeric choline, specifically [2-(methacryloyloxy)ethyl]-trimethylammonium chloride (TMAMA), underwent biofunctionalization through an ion exchange reaction with the model drug anion: -aminosalicylate (PAS), a primary antibiotic for tuberculosis treatment. This modified biocompatible IL monomer (TMAMA/PAS) was subsequently copolymerized with methyl methacrylate (MMA) to directly synthesize the well-defined graft conjugates with regulated content of ionic fraction with PAS anions (up to 49%), acting as drug delivery systems. The length of the polymeric side chains was assessed by the monomer conversions, yielding a degree of polymerization ranging from 12 to 89. The density of side chains was controlled by "grafting from" using the multifunctional macroinitiators. In vitro drug release, triggered by the ion exchange between the pharmaceutical and phosphate anions in a PBS medium, occurred in the range of 71-100% (2.8-9.8 μg/mL). Owing to significant drug content and consistent release profiles, these particular graft copolymers, derived from biomodified IL monomers with ionically attached pharmaceutical PAS in the side chains, are recognized as potentially effective drug delivery vehicles.
一种基于单体胆碱的离子液体,具体为[2-(甲基丙烯酰氧基)乙基]-三甲基氯化铵(TMAMA),通过与模型药物阴离子:对氨基水杨酸盐(PAS,一种治疗结核病的主要抗生素)进行离子交换反应实现生物功能化。这种经过修饰的生物相容性离子液体单体(TMAMA/PAS)随后与甲基丙烯酸甲酯(MMA)共聚,以直接合成具有可控离子部分含量(高达49%)的明确接枝共轭物,用作药物递送系统。通过单体转化率评估聚合物侧链的长度,聚合度范围为12至89。侧链密度通过使用多功能大分子引发剂的“从接枝”方法进行控制。在PBS介质中,药物与磷酸根阴离子之间的离子交换引发体外药物释放,释放范围为71 - 100%(2.8 - 9.8μg/mL)。由于显著的药物含量和一致的释放曲线,这些源自侧链带有离子连接药物PAS的生物修饰离子液体单体的特定接枝共聚物被认为是潜在有效的药物递送载体。