title: Optimization of paeonol-loaded poly(butyl-2-cyanoacrylate) nanocapsules by central composite design with response surface methodology together with the antibacterial properties.
abstract: 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 (R2and adjusted R2were 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±1.20nm). 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.
authors.affiliation: International Joint Lab of Tea Chemistry and Health Effects, State Key Laboratory of Tea Plant Biology and Utilization, Anhui Agricultural University, 130 West Changjiang Road, Hefei, Anhui Province 230036, China; School of Life Sciences, Anhui Agricultural University, Hefei 230036, China.
authors.forename: Jingjing
authors.initials: J
authors.lastname: Yao
authors.affiliation: School of Life Sciences, Anhui Agricultural University, Hefei 230036, China.
authors.forename: Yangxin
authors.initials: Y
authors.lastname: Zhang
authors.affiliation: International Joint Lab of Tea Chemistry and Health Effects, State Key Laboratory of Tea Plant Biology and Utilization, Anhui Agricultural University, 130 West Changjiang Road, Hefei, Anhui Province 230036, China.
authors.forename: Qiming
authors.initials: Q
authors.lastname: Hu
authors.affiliation: School of Life Sciences, Anhui Agricultural University, Hefei 230036, China.
authors.forename: Decheng
authors.initials: D
authors.lastname: Zeng
authors.affiliation: International Joint Lab of Tea Chemistry and Health Effects, State Key Laboratory of Tea Plant Biology and Utilization, Anhui Agricultural University, 130 West Changjiang Road, Hefei, Anhui Province 230036, China.
authors.forename: Fang
authors.initials: F
authors.lastname: Hua
authors.affiliation: School of Life Sciences, Anhui Agricultural University, Hefei 230036, China.
authors.forename: Wei
authors.initials: W
authors.lastname: Meng
authors.affiliation: School of Life Sciences, Anhui Agricultural University, Hefei 230036, China. Electronic address: weiywswzy@163.com.
authors.forename: Weiyun
authors.initials: W
authors.lastname: Wang
authors.affiliation: International Joint Lab of Tea Chemistry and Health Effects, State Key Laboratory of Tea Plant Biology and Utilization, Anhui Agricultural University, 130 West Changjiang Road, Hefei, Anhui Province 230036, China. Electronic address: baoguanhu@ahau.edu.cn.
authors.forename: Guan-Hu
authors.initials: GH
authors.lastname: Bao
mesh_terms: D000098:Acetophenones / Q000737:chemistry*; D000900:Anti-Bacterial Agents / Q000737:chemistry*; D001682:Biological Availability; D002626:Chemistry, Pharmaceutical; D004659:Enbucrilate / Q000737:chemistry*; D053769:Nanocapsules / Q000737:chemistry*; D053758:Nanoparticles / Q000737:chemistry; D010316:Particle Size; D020442:Poloxamer / Q000737:chemistry; D011108:Polymers / Q000737:chemistry*; D013499:Surface Properties
chemical_list: D000098:Acetophenones; D000900:Anti-Bacterial Agents; D053769:Nanocapsules; D011108:Polymers; D020442:Poloxamer; C013638:paeonol; D004659:Enbucrilate
keywords: Antibacterial; Central composite design; Nanocapsules; Optimization; Paeonol