Jelonek Katarzyna, Musiał-Kulik Monika, Pastusiak Małgorzata, Foryś Aleksander, Zięba Andrzej, Kasperczyk Janusz
Centre of Polymer and Carbon Materials, Polish Academy of Sciences, 34 Curie-Skłodowskiej St., 41-819 Zabrze, Poland.
Department of Organic Chemistry, Faculty of Pharmaceutical Sciences in Sosnowiec, Medical University of Silesia, 4 Jagiellońska St., 41-200 Sosnowiec, Poland.
Pharmaceutics. 2024 Dec 16;16(12):1597. doi: 10.3390/pharmaceutics16121597.
: Cancer remains one of the leading causes of death worldwide, and thus, there is a need for the development of innovative and more effective treatment strategies. The aim of the study was to evaluate two types of nanoparticles-nanospheres and micelles-obtained from PLA-based polymers to discover their potential for delivering four types of phenothiazine derivatives. : The morphology, drug-loading properties, cytocompatibility, hemolytic properties and anticancer activity were analyzed. : The micelles exhibited significantly higher drug-loading properties, release process and cytotoxic activity against cancer cells compared to the nanospheres. The micelles containing 5-methyl-12-quino[3,4-][1,4]benzothiazinium chloride with an OH group as a substituent in the 10-position of the quinobenzothiazine ring showed the highest drug-loading content, the most efficient drug release, the lowest hemolytic activity and the most significant cytotoxic effect against HeLa cells. : The conducted study enabled the development of a delivery system for the new anticancer compound and showed that the choice of drug carrier has a crucial effect on its cytotoxic potential against cancer cells.
癌症仍然是全球主要死因之一，因此，需要开发创新且更有效的治疗策略。本研究的目的是评估从基于聚乳酸的聚合物中获得的两种类型的纳米颗粒——纳米球和胶束，以发现它们递送四种吩噻嗪衍生物的潜力。分析了其形态、载药性能、细胞相容性、溶血性能和抗癌活性。与纳米球相比，胶束表现出显著更高的载药性能、释放过程和对癌细胞的细胞毒性活性。在喹啉并苯并噻嗪环的10位带有OH基团作为取代基的含5-甲基-12-喹啉并[3,4-][1,4]苯并噻嗪氯化物的胶束显示出最高的载药含量、最有效的药物释放、最低的溶血活性以及对HeLa细胞最显著的细胞毒性作用。所进行的研究促成了一种新型抗癌化合物递送系统的开发，并表明药物载体的选择对其对癌细胞的细胞毒性潜力具有关键影响。
