Derivatization of Some Maleic Anhydride Containing Copolymers with Amine Functionalized Pharmaceutical Active Substances, Structural Characterizations and Biological Activities

Karakus G.

MARMARA PHARMACEUTICAL JOURNAL, vol.19, no.2, pp.121-125, 2015 (Journal Indexed in ESCI) identifier identifier

  • Publication Type: Article / Article
  • Volume: 19 Issue: 2
  • Publication Date: 2015
  • Doi Number: 10.12991/mpj.20151910458
  • Page Numbers: pp.121-125


Poly(maleic anhydride-co-styrene) (MAST), poly(maleic anhydride-co-vinyl acetate) (MAVA), poly(maleic anhydride-co-methyl methacrylate) (MAMMA), poly(maleic anhydride-co-allyl phenyl ether) (MAAFE) and poly(maleic anhydride-alt-acrylic acid) (MAAA) copolymers were synthesized by free radical chain polymerization reaction. Modification/derivatization of the copolymers with active pharmaceutical ingredients, in amine form (-NH2), was performed by the ring opening reaction. Structural characterization of the copolymers and the conjugated products was carried out by Fourier Transform Infrared (FTIR) and Nuclear Magnetic Resonance (H-1-NMR). The FTIR and H-1-NMR spectra, confirmed that pharmaceutically active agents were covalently bonded to the MAVA copolymer in a succesfull manner. Furthermore cytotoxicity on healthy fibroblast cell lines, antiproliferative activity on cancer cell lines and antibacterial activity on bacterial strains were also investigated in-vitro for synthesized conjugates. MAVA copolymer was also selected the most suitable carrier for modification/derivaritization process by comparing its affinity to the pharmaceutically active agents.