Marmara Pharmaceutical Journal 2015 , Vol 19 , Issue 2
Derivatization of Some Maleic Anhydride Containing Copolymers with Amine Functionalized Pharmaceutical Active Substances, Structural Characterizations and Biological Activities
Gulderen KARAKUS1
1Cumhuriyet Üniversitesi, Eczacılık Fakültesi, Farmasötik Kimya Anabilim Dalı, Sivas 58140, Türkiye DOI : 10.12991/mpj.20151910458 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 (1H-NMR). The FTIR and 1H-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. Keywords : Copolymer modification, ring opening reaction, antiproliferative activity, antibacterial activity, structural characterization