title: Synthesis and characterization of pH-sensitive conjugate of isoniazid--methoxypoly(ethylene glycol)-b-poly(L-lysine).
abstract: The present paper deals with the preparation and characterization of a conjugate of isoniazid (INH) with the block copolymer methoxypoly(ethylene glycol)-b-poly(L-lysine) (mPEG-b-PLL). The structure of the conjugate (mPEG-b-PLL-INH) was verified by means of (1)H NMR, GPC, infrared spectroscopy, elemental analysis and powder X-ray diffraction. The conjugate contains six l-lysine units with five INH molecules, which are attached by means of pH-sensitive amidine bond. Under in vitro conditions, the conjugate is hydrolyzed and isoniazid is released (pH 4; 37 °C; t(1/2) ≈ 10 h).
authors.affiliation: Institute of Organic Chemistry and Technology, University of Pardubice, Studentská 573, 532 10 Pardubice, Czech Republic. ales.imramovsky@upce.cz
authors.forename: Aleš
authors.initials: A
authors.lastname: Imramovský
authors.forename: Ludmila
authors.initials: L
authors.lastname: Grusová
authors.forename: Ludvík
authors.initials: L
authors.lastname: Beneš
authors.forename: Vladimír
authors.initials: V
authors.lastname: Pejchal
authors.forename: Miloš
authors.initials: M
authors.lastname: Sedlák
mesh_terms: D006863:Hydrogen-Ion Concentration; D007538:Isoniazid / Q000737:chemistry*; D015394:Molecular Structure; D011092:Polyethylene Glycols / Q000737:chemistry*; D011107:Polylysine / Q000031:analogs & derivatives* / Q000737:chemistry; D033362:Powder Diffraction
chemical_list: C117924:mPEG-block-PLL; D011107:Polylysine; D011092:Polyethylene Glycols; D007538:Isoniazid