Enhanced efficacy of baicalin-loaded TPGS polymeric micelles against periodontitis

As a chronic infectious disease, periodontitis is the main cause of teeth exfoliation due to its severe inflammatory reaction and periodontal tissue destruction. Recent reports have shown that baicalin could inhibit the NF-κB signaling pathway in inflammatory activity of periodontitis, but the efficacy of baicalin is limited due to its poor water solubility. In this work, we report the fabrication and application of baicalin encapsulated D-α-tocopherol polyethylene glycol 1000 succinate (TPGS) polymeric micelles (PMs) through thin-film hydration method. The monodispersed micelles showed a spherical shape in aqueous solution and a prolonged drug-release kinetic. After baicalin was loaded into PMs, cytotoxicity and apoptosis induction were both decreased. The expression of genes (including TNF-α, IL-1β, RANKL and NF-κB) and the phosphorylation level of NF-κB p65 protein in lipopolysaccharide (LPS)-induced rat gingival fibroblasts were also reduced. Further investigation of drug efficacy in a rat periodontal disease model confirmed that the use of baicalin-PMs could reduce the destruction of alveolar bone and gingival fiber. Moreover, the therapeutic effect of baicalin-PMs was significantly better than that of free baicalin. These results suggest that the direct injection of micelles containing water-insoluble drugs may become a simple but effective method for treating periodontitis. [Display omitted] •Sub-30 nm baicalin-loaded polymeric micelles were successfully synthesized by thin-film hydration method.•Compared with free drugs, baicalin-loaded micelles showed less cytotoxicity to cell proliferation.•Baicalin-loaded micelles significantly suppressed the development of periodontitis through NF- κB signaling pathway.•Rat periodontitis model proved the treatment efficacy of baicalin-loaded micelles.