Optimization of Preparation Technology for Paeonol Proniosomes by Central Composite Design-Response Surface Methodology and Investigation of Its in vitro Percutaneous Permeability

Abstract:

Objective: To optimize formulation of paeonol proniosomes and investigate its transdermal performance. Method: Taking quality of cholesterol,soybean lecithin and span-60 as independent variables,average particle size and entrapment efficiency as dependent variable,various levels of independent variables were fitted by binomial equation,response surface methodology was used to optimize formulation,prediction was carried out through comparing the observed and predicted value.Franz diffusion cell test was adopted by taking physiological saline as acceptable liquid and nude mouse skin as membrane,HPLC was adopted to determine the content of paeonol,steady state permeation rate(J_s) and unit area cumulative percutaneous penetration amount(Q) of paeonol proniosomes,paeonol proniosomes oinements and ordinary ointments were compared. Result: Optimum formulation was as follows:cholesterol 7.53 mg,soybean lecithin 107.86 mg,span-60 74.49 mg, peaonol 5 mg;Encapsulation efficiency of these prepared paeonol proniosomes was 64.16%,average particle size was 11.15 μm,binomial model fitting was good.Q12 of paeonol proniosomes,paeonol proniosomes ointments and ordinary ointments were (125.54±8.87),(96.20±5.87),(75.83±18.42) μg·cm^-2,J_s were 10.327, 7.826,5.967 μg·cm^-2·h^-1,respectively. Conclusion: Central composite design-response surface methodology could accurately reflect interaction of multiple factors and levels,which was suitable for optimizing formulation.Penetration capacity of paeonol proniosomes and paeonol proniosomes ointments were higher than ordinary ointments.