Preparation and characterization of nintedanib nano-liposomes

Abstract

Objective To investigate the key physical and chemical properties of nintedanib liposomes prepared by 4 different methods in order to screen out the best preparation method of nintedanib liposomes. Methods Firstly, nintedanib liposomes were prepared by thin film dispersion, reverse evaporation, ethanol injection and modified ethanol injection, respectively. The entrapment efficiency of nintedanib liposomes was then determined by dialysis and characterized for particle size, dispersibility, surface potential, and morphology. Their stability was evaluated after being placed at room temperature for 7 d. Results Circular nintedanib liposomes were respectively prepared by thin film dispersion, reverse evaporation, ethanol injection and modified ethanol injection, with a particle size of (285.1±12.3), (271.4±5.9), (226.3±14.8) and (197.2±11.2) nm, an encapsulation rate of (15.82±1.26)%, (16.71±1.35)%, (25.12±3.21)% and (32.5±3.61)%, respectively. The nintedanib liposomes prepared by modified ethanol injection had significantly smallest particle size and highest encapsulation efficiency than the liposomes by the other 3 methods (P 0.05). Conclusion Nintedanib liposomes prepared by modified ethanol injection have excellent key physical and chemical properties, and this method is an optical one for preparing nintedanib liposomes.

Keywords

• nintedanib esylate
• liposome
• particle sizes
• ethanol injection method