Optimization of paeonol-loaded poly(butyl-2-cyanoacrylate) nanocapsules by central composite design with response surface methodology together with the antibacterial properties

    loading  Checking for direct PDF access through Ovid


With the aim to enhance dissolution rate and bioavailability of paeonol, paeonol-loaded poly(butyl-2-cyanoacrylate) nanocapsules (Pae@PNCs) were prepared by interfacial spontaneous polymerization for the first time. Herein, a rotatable central composite design (RCCD) with three-factor five-level was applied to evaluate the optimization experiments. To the maximum percentage encapsulation efficiency (EE%) and minimum particle size (nm) of the Pae@PNCs, a quadratic polynomial model was generated to predict and evaluate the independent variables with respect to the dependent variables. RSM model goodness fitting were confirmed by the ANOVA Table (P < 0.05) through variance analysis, which predicted values of EE (%) and particle size (R2 and adjusted R2 were close to 1, respectively) in good agreement with experimental values. By solving the regression equation and analyzing the response surface, three-dimensional model graphs and plots, the optimal result for the preparation of Pae@PNCs were found to be: pH (2.34), Poloxamer F-68 (0.80% m/v) and ethyl acetate/α-BCA ratio (16.67 v/v) for the highest EE% (73.58 ± 2.76%) and the smallest particle size (42.06 ± 1.20 nm). The release profiles and antibacterial activity in vitro from the optimal Pae@PNCs were performed. The results indicated that it has slow and well-controlled release, and has strong antibacterial activity in vitro than paeonol. This understanding can help to predict the conditions of optimization of poly(butyl-2-cyanoacrylate) nanoparticles formation and to improve paeonol bioavailability and pharmacological properties.

Graphical abstract

Here, we report the preparation of Paeonol-loaded poly(butyl-2-cyanoacrylate) nanocapsules (Pae@PNCs) by interfacial spontaneous polymerization. The response surface methodology (RSM) in a rotatable central composite design (RCCD) has also been successfully applied to optimize the experimental conditions for drug delivery systems, which optimize preparation Pae@PNCs with highest EE% (73.58 ± 2.76%), the smallest particle size (42.06 ± 1.20 nm) and homogeneous distribution. Finally, the release profiles and antibacterial activity in vitro from optimal Pae@PNCs were also performed.

Related Topics

    loading  Loading Related Articles