Optimization of the Matrix Formulation of Sanse Powder Gel Paste and Its Intervention Effect on Synovitis in KOA Rats

  OBJECTIVE  In order to optimize the matrix formulation of Sanse Powder gel paste and to study its anti-synovitis effect on KOA rats.

  METHODS  The comprehensive sensory, initial adhesive strength, holding adhesive strength and peel strength were used as evaluation indexes. Sodium polyacrylate, aluminum glycolate, tartaric acid and glycerol were used as investigation factors. The optimal matrix formulation was screened by orthogonal test. Subsequently, the rats were randomly divided into blank group, model group, Sanse Powder gel paste group, Sanse Powder traditional preparation group and Sanse Powder gel paste (containing penetration enhancers). Except blank group, the modified Hulth method was used to establish the KOA model. After the model was established successfully, plaster was applied externally in each administration group for 28 days. Synovial tissues were extracted from each group after the final administration. Synovitis was assessed by HE staining and synovial collagen deposition was assessed by sirius red staining. Protein and mRNA expressions of IL-1β, TNF-α and IL-6 in synovium were detected by Western blot and qPCR.

  RESULTS  The optimal matrix formulation of the Sanse Powder gel paste was sodium polyacrylate (50 g), aluminium glycolate (2.5 g), tartaric acid (3 g), glycerol (500 g), Sanse Powder (150 g), pure water (50 mL) and carbomer (120 g). After 28 days of drug administration, HE and sirius red staining of synovial tissues results showed that, compared with model group, the inflammatory cell infiltration, collagen deposition and synovial fibrosis in the Sanse Powder gel paste group and the Sanse Powder traditional preparation group decreased, the protein and mRNA expressions of IL-1β, TNF-α and IL-6 were reduced in the Sanse Powder gel paste group and the Sanse Powder traditional preparation group (P < 0.01). Compared with Sanse Powder traditional preparation group, there was no significant difference in the protein expressions of IL-1β, TNF-α and IL-6 in the Sanse Powder gel paste group, the mRNA expressions of IL-1β and IL-6 were significantly lower in the Sanse Powder gel paste group (P < 0.05), while there was no significant difference in TNF-α mRNA expression. Compared with the Sanse Powder gel paste group, the protein expression of IL-1β was reduced in the Sanse Powder gel paste (containing penetration enhancers) (P < 0.01), while there was no significant difference in protein expressions of TNF-α and IL-6. However, compared with the Sanse Powder gel paste group, the Sanse Powder gel paste (containing penetration enhancers) significantly inhibited the mRNA expressions of IL-1β, TNF-α and IL-6 (P < 0.05, P < 0.01).

  CONCLUSION  The optimized matrix formulation is stable and feasible, and the operation method is simple. The Sanse Powder gel paste has good appearance and adhesion, and can effectively reduce the synovitis of KOA rats. The addition of osmotic enhancer can enhance the anti-inflammatory effect of Sanse Powder gel paste, which provide reference for further research.