Abstract

In the framework of this investigation novel modified liposomal formulations based on 1,2-dipalmitoyl-sn-glycero-3-phosphocholine (DPPC) and hydroxyethylated imidazolium-containing amphiphiles with various length of hydrophobic tail have been fabricated and characterized by various physicochemical methods. Variation of amphiphile/lipid molar ratio has been used as a tool for optimization of the composition of obtained liposomes. It has been revealed, that modification of DPPC liposomes by these amphiphiles results in increase of the stability of formulation, which could be extended from 2 weeks up to 5 months. Obtained liposomes have been used for encapsulation of hydrophilic cargos – antibiotic chloramphenicol and anticancer drug cisplatin and their in vitro release profiles have been evaluated. Liposomal formulation of chloramphenicol has been tested for hemolytic activity, which allowed to demonstrate its 4-fold lower toxicity in comparison with individual amphiphile of the same concentration. Examination of liposomal formulation of cisplatin against HeLa cancer cells has revealed, that encapsulated drug is more effective, than free one by about 5 times. Using confocal microscopy technique, it has been shown, that modification of liposomes with a hydroxyethylated imidazolium amphiphiles results in targeted delivery of encapsulated compounds to mitochondria.

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