Nanoparticles as Potential Delivery System of Phenothiazine Derivatives for Anticancer Application

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Abstract

Cancer remains a one of a leading cause of death worldwide, and thus there is a need for the de-velopment 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 pol-ymers for discovering their potential for delivery of four types of phenothiazine derivatives. The morphology, drug loading properties, cytocompatibility, hemolytic properties and anti-cancer activity has been analyzed. The micelles exhibited significantly higher drug loading properties, release process and cytotoxic activity against cancer cells compared to the nano-spheres. The micelles containing 5-methyl-12H-quino[3,4-b][1,4]benzothiazinium chloride with OH group as substituent in 10-position of the quinobenzothiazine ring showed the highest drug loading content, the most efficient drug release, the lowest hemolytic activity and the most sig-nificant cytotoxic effect against HeLa cells. The conducted study enabled to develop 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.

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