Poly(ethylene oxide)‐g‐gellan polysaccharide nanocarriers for controlled gastrointestinal delivery of simvastatin

Herein, a novel gellan polysaccharide‐based amphiphilic copolymer was synthesized for the development of simvastatin‐loaded micellar nanoparticles. The nanoparticles were explored for their controlled drug release and improved pharmacodynamic potentials. The copolymer was characterized by Fourier transform infrared spectroscopy (FTIR) and elemental analysis. The onset of copolymer micellization was detected by fluorescence spectroscopy. Simvastatin was loaded into micellar particles by solvent evaporation method and the particles were then characterized by microscopic and light scattering techniques. The physical state of drug was studied by X‐ray diffraction analysis. Pharmacodynamic assessment of the micellar preparations was done on rabbit models. The copolymer formed micellar nanoparticles in water. Critical micellar concentration was 9.12mg/l. The micellar particles (426.8–912.6nm) entrapped a maximum of 18.86% drug. Higher negative zeta potential indicated physical stability of micellar systems. A simple diffusion mechanism was operative in the event of comparatively faster drug release in pH6.8 phosphate buffer solution. No significant drug‐copolymer interaction was traced by FTIR spectroscopy. The amorphization of drug into micellar particles reduced LDL‐cholesterol level by ～45% in hyperlipidemic rabbits and this was about 2.5 times higher than pure drug dispersion. Copolymer micellar nanoparticles of simvastatin could control cholesterol level in hyperlipidemic rabbits and thus had potential in drug delivery applications. © 2015 Wiley Periodicals, Inc. J. Appl. Polym. Sci. 2015 , 132, 42399.