Preparation, characterization and evaluation of the in vivo trypanocidal activity of ursolic acid-loaded solid dispersion with poloxamer 407 and sodium caprate

摘要: Ursolic acid is a promising candidate for treatment of Chagas disease; however it has low aqueous solubility and intestinal absorption, which are both limiting factors bioavailability. Among the strategies to enhance dissolution lipophilic drugs, solid dispersions growing in popularity. In this study, we employed mixture surfactants poloxamer 407 with sodium caprate produce dispersion containing ursolic aimed at enhancing drug vivo trypanocidal activity. Compared physical mixture, presented higher bulk density smaller particle size. Fourier Transform Infrared Spectroscopy results showed hydrogen bonding intermolecular interactions between 407. X-ray diffractometry experiments revealed conversion from its crystalline form more soluble amorphous structure. Consequently, was increased dissolved fast complete manner. Taken together oral absorption-enhancing property caprate, these explained increase activity dispersion, also proved be safe by cytotoxicity evaluation using LLC-MK2 cell line.