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


Karakus G.

MARMARA PHARMACEUTICAL JOURNAL, cilt.19, ss.121-125, 2015 (ESCI İndekslerine Giren Dergi) identifier identifier

  • Cilt numarası: 19 Konu: 2
  • Basım Tarihi: 2015
  • Doi Numarası: 10.12991/mpj.20151910458
  • Dergi Adı: MARMARA PHARMACEUTICAL JOURNAL
  • Sayfa Sayıları: ss.121-125

Özet

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.