Preparation, characterisation and in vitro anti-inflammatory activity of Baicalin microsponges
Miao Li,
Jiajie Gan,
Xuhui Xu,
Shuai Zhang,
Yuanyuan Li,
Le Bian,
Zibo Dong
Affiliations
Miao Li
School of Pharmacy, Jiangsu Ocean University, Lianyungang, 222005, PR China; Jiangsu Key Laboratory of Marine Pharmaceutical Compound Screening, Lianyungang, 222005, PR China
Jiajie Gan
School of Pharmacy, Jiangsu Ocean University, Lianyungang, 222005, PR China; Jiangsu Marine Pharmaceutical Resources Development Engineering Research Center, Lianyungang, 222005, PR China
Xuhui Xu
School of Pharmacy, Jiangsu Ocean University, Lianyungang, 222005, PR China; Jiangsu Key Laboratory of Marine Pharmaceutical Compound Screening, Lianyungang, 222005, PR China
Shuai Zhang
School of Pharmacy, Jiangsu Ocean University, Lianyungang, 222005, PR China; Jiangsu Marine Pharmaceutical Resources Development Engineering Research Center, Lianyungang, 222005, PR China
Yuanyuan Li
School of Pharmacy, Jiangsu Ocean University, Lianyungang, 222005, PR China
Le Bian
School of Pharmacy, Jiangsu Ocean University, Lianyungang, 222005, PR China; Jiangsu Marine Pharmaceutical Resources Development Engineering Research Center, Lianyungang, 222005, PR China
Zibo Dong
School of Pharmacy, Jiangsu Ocean University, Lianyungang, 222005, PR China; Jiangsu Key Laboratory of Marine Pharmaceutical Compound Screening, Lianyungang, 222005, PR China; Jiangsu Marine Pharmaceutical Resources Development Engineering Research Center, Lianyungang, 222005, PR China; Corresponding author. School of Pharmacy, Jiangsu Ocean University, Lianyungang, 222005, PR China.
Baicalin, a flavonoid extracted from traditional Chinese medicine, Scutellaria baicalensis has significant anti-inflammatory effects. Microsponges are drug delivery systems that improve drug stability and slow the release rate. The combination of baicalin and the microsponges produced a new and stable system for its delivery, resulting in a novel formulation of baicalin. Baicalin microsponges (BM) were prepared using the quasi-emulsion solvent diffusion method. Effects of the mass ratio of the polymer (ethylcellulose) to baicalin, the concentration of the emulsifier polyvinyl alcohol (PVA), the stirring speed on the encapsulation efficiency (EE), and yield of the microsponges were investigated by combining the one-factor test and Box-Behnken design (BBD). The preparation process was standardised using 2.61:1 mass ratio of ethyl cellulose to baicalin, 2.17% concentration of PVA, with stirring at 794 rpm. Optimised BM formulations were evaluated for the parameters of EE (54.06 ± 3.02)% and yield of (70.37 ± 2.41)%, transmission electron microscopy (TEM), and in vitro cell evaluation. Results of the in vitro anti-inflammatory assay showed that baicalin microsponges-pretreated-lipopolysaccharide (LPS)-induced RAW264.7, mouse macrophages showed reduced inflammatory response, similar to that seen in baicalin-treated macrophages.