Novel polymeric derivatives of betulin with anticancer activity.

ABSTRACT: In order to provide novel polymeric biomaterials for chemotherapeutic purposes, in this paper we described the synthesis and the characterization of the physicochemical properties of a betulin-based polyanhydride exhibiting anti-cancer effects. The polyanhydride was obtained by a melt polycondensation of a disuccinate betulin (3,28-di-O-succinyl betulin), and was thoroughly characterized through ¹H NMR and ¹³C NMR spectroscopies, correlation spectroscopy, heteronuclear single quantum correlation, size exclusion chromatography, differential scanning calorimetry and FT-IR spectroscopy. It was confirmed, that the obtained polyanhydride undergoes hydrolytic degradation, releasing disuccinate betulin as a degradation product. Polyanhydride of a disuccinate betulin was tested for cytostatic activity against a wide range of cancer cell lines (HeLa, MCF-7, A-549, U-87MG, KB and HepG2), proving its efficiency in inhibiting the growth of selected cancer cells. To realize the concept of an easily administrated drug release system, polyanhydride was fabricated in a form of micro- (1-30 μm) and nanospheres (∼400 nm) by using an emulsion solvent evaporation method. The micro- and nanospheres were characterized by SEM.

SUBMITTER: Niewolik D 

PROVIDER: S-EPMC9065995 | biostudies-literature | 2019 Jul

REPOSITORIES: biostudies-literature