ABSTRACT
A Box-Behnken design with three replicates was used for preparation and evaluation of Eudragit vancomycin [VCM] nanoparticles prepared by double emulsion. The purpose of this work was to optimize VCM nanoparticles to improve the physicochemical properties. Nanoparticles were formed by using W1/O/W2 double-emulsion solvent evaporation method using Eudragit RS as a retardant material. Full factorial design was employed to study the effect of independent variables, RPM [X1], amount of emulsifier [X2], stirring rate [X3], volume of organic phase [X4] and volume of aqueous phase [X5], on the dependent variables as production yield, encapsulation efficiency and particle size. The optimum condition for VCM nanoparticles preparation was 1:2 drug to polymer ratio, 0.2 [%w/w] amount of emulsifier, 25 mL [volume of organic phase], 25 mL [volume of aqueous phase], 3 min [time of stirring] and 26000 RPM. RPM and emulsifier concentrations were the effective factors on the drug loading [R2 = 90.82]. The highest entrapment efficiency was obtained when the ratio of drug to polymer was 1:3. Zeta [zeta] potential of the nanoparticles was fairly positive in molecular level. In vitro release study showed two phases: an initial burst for 0.5 h followed by a very slow release pattern during a period of 24 h. The release of VCM was influenced by the drug to polymer ratio and particle size and was found to be diffusion controlled. The best-fit release kinetic was achieved with Peppas model. In conclusion, the VCM nanoparticle preparations showed optimize formulation, which can be useful for oral administrations