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Issue 36, 2019, Issue in Progress
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Novel polymeric derivatives of betulin with anticancer activity

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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.

Graphical abstract: Novel polymeric derivatives of betulin with anticancer activity

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Publication details

The article was received on 04 May 2019, accepted on 24 Jun 2019 and first published on 04 Jul 2019


Article type: Paper
DOI: 10.1039/C9RA03326B
RSC Adv., 2019,9, 20892-20900
  • Open access: Creative Commons BY-NC license
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    Novel polymeric derivatives of betulin with anticancer activity

    D. Niewolik, K. Krukiewicz, B. Bednarczyk-Cwynar, P. Ruszkowski and K. Jaszcz, RSC Adv., 2019, 9, 20892
    DOI: 10.1039/C9RA03326B

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