Keihankhadiv Shadi, Neugebauer Dorota
Department of Physical Chemistry and Technology of Polymers, Faculty of Chemistry, Silesian University of Technology, 44-100 Gliwice, Poland.
Pharmaceuticals (Basel). 2023 Oct 23;16(10):1502. doi: 10.3390/ph16101502.
Bioactive linear choline-based copolymers were developed as micellar carriers for drug delivery systems (DDSs). The polymethacrylates containing trimethylammonium groups with -aminosalicylate anions (PAS-based copolymers: series 1) or chloride anions (Cl-based copolymers: series 2) differing in ionic content and chain length were selected for drug loading. The diverse structures of amphiphilic copolymers made it possible to adjust the encapsulation efficiency of a well-known antibiotic, i.e., -aminosalicylate in the form of sodium salt (PASNa) or acid (PASA), providing single drug systems. Goniometry was applied to verify the self-assembly capacity of the copolymers using the critical micelle concentration (CMC = 0.03-0.18 mg/mL) and the hydrophilicity level quantifying the surface wettability of polymer film using the water contact angle (WCA = 30-53°). Both parameters were regulated by the copolymer composition, indicating that the increase in ionic content caused higher CMC and lower WCA, but the latter was also modified to a less hydrophilic surface by drug encapsulation. The drug content (DC) in the PAS-based polymers was increased twice by encapsulation of PASNa and PASA (47-96% and 86-104%), whereas in the chloride-based polymer systems, the drug was loaded in 43-96% and 73-100%, respectively. Efficient drug release was detected for PASNa (80-100% series 1; 50-100% series 2) and PASA as complete in both series. The strategy of loading extra drug by encapsulation, which enhances the drug content in the copolymers containing anions of the same pharmaceutics, provided promising characteristics, which highlight the potential of PAS-loaded micellar copolymers for drug delivery.
生物活性线性胆碱基共聚物被开发用作药物递送系统（DDS）的胶束载体。选择含有带 - 氨基水杨酸盐阴离子的三甲基铵基团的聚甲基丙烯酸酯（基于PAS的共聚物：系列1）或离子含量和链长不同的氯化物阴离子（基于Cl的共聚物：系列2）用于药物负载。两亲共聚物的多样结构使得调节一种知名抗生素即钠盐形式（PASNa）或酸形式（PASA）的 - 氨基水杨酸盐的包封效率成为可能，从而提供单药系统。应用测角法使用临界胶束浓度（CMC = 0.03 - 0.18 mg/mL）验证共聚物的自组装能力，并使用水接触角（WCA = 30 - 53°）定量聚合物膜的表面润湿性来表征亲水性水平。这两个参数均由共聚物组成调节，表明离子含量的增加导致更高的CMC和更低的WCA，但药物包封也使后者转变为亲水性较低的表面。通过包封PASNa和PASA，基于PAS的聚合物中的药物含量（DC）增加了两倍（47 - 96%和86 - 104%），而在基于氯化物的聚合物系统中，药物负载率分别为43 - 96%和73 - 100%。检测到PASNa（系列1为80 - 100%；系列2为50 - 100%）和PASA在两个系列中均能有效释放且完全释放。通过包封额外负载药物的策略提高了含有相同药物阴离子的共聚物中的药物含量，展现出有前景的特性，突出了负载PAS的胶束共聚物在药物递送方面的潜力。
