Hexadecyl gellan amphiphilic nanoparticles: Physicochemical properties and in vivo lipid-lowering potential

Abstract

Herein, an amphiphilic hexadecyl gellan copolymer was synthesized and characterized by FTIR, elemental analysis and its degree of substitution. The copolymer self-assembled in water and formed spherical nanostructures. Simvastatin was loaded into micelles by solvent evaporation method. The critical association concentration of the copolymer was 0.63 mg/l. The micellar system showed negative zeta potentials (−27.4 to −28.2 mV). Copolymer micellization caused ∼355 fold increase in solubility of the drug in water. The dissolution efficiency of micellar system was higher in phosphate buffer solution (pH6.8) than in acidic solution (pH1.2). The nanoparticles released only 60% drug in phosphate buffer solution at the end of 8 h. The drug release followed anomalous diffusion mechanism. The nanoparticles reduced LDL-cholesterol level by 69.04% after 18 h of oral administration into rabbits. Thus, the hexadecyl gellan copolymer particles could be useful in controlling drug release rate and lowering LDL-cholesterol level over an extended period.