Preparation Of Ketoconazole-Loaded Polybutylcyanoacry Late Nanoparticles

Objective:To preparation and evaluation the Ketoconazole-loaded polybutylcyanoacrylate (KTZ-PBCA), nanoparticles and determination the pharmacodynamics efficacy.Method:The KTZ-PBCA nanoparticles were prepared by interfacial polymerization method. The L9(34) orthogonal design test was used to optimize the preparation method. The entrapment efficiency of Ketoconazole was used as the control index, and the mass ratio of drugs and poloxamer, drugs and Dextranum, drugs and a-BCA, and the pH value were used as investigating factors. The drug content was determined by HPLC method. The in vitro transdermal efficiency was evaluated by TP-5intelligent transdermal diffusion instrument. And the in vitro antibacterial activity of KTZ-PBCA nanoparticles was investigated by tube double dilution method and paper diffusion method. Using frosted preparing guinea pigs ringworm of the body model to study the efficacy of KTZ-PBCA nanoparticles.Result:The optimum preparation process of KTZ-PBCA nanoparticles:the mass ratio of KTZ and poloxamer was1:4, the mass ratio of KTZ and Dextranum was1:4, the mass ratio of KTZ and a-BCA was1:5(mg:ug), pH value is1.0. Its average of encapsulation efficiency was78.85%, the average diameter was33.7nm, the Zeta value was32.76mV. KTZ-PBCA nanoparticles’s steady-state transdermal efficiency was9.995μg-cm-2-h-1, the cream preparation’s transdermal teady-state transdermal efficiency is5.208μg-cm-2-h-1. KTZ-PBCA nanoparticles’s transdermal effect is stronger than the cream preparation. In vitro bacteriostasis experiment by tube double dilution method and paper diffusion method indicate that KTZ-PBCA nanoparticles has obvious bacteriostatic effect than cream preparation. Pharmacodynamic experiment shows that KTZ-PBCA nanoparticles has good curative effect on mice models, compared with positive group there was no statistically significant difference.Conclusion:KTZ-PBCA nanoparticles technology is simple and feasible, the drugs have the effect of percutaneous penetration and have no irritating to the skin. KTZ-PBCA nanoparticles and ream preparation have same effect on mice models, moreover have evident effect on the infected Candida albicans skin of mice.