A designed self-microemulsifying delivery system: Stability and Anti-inflammation in vivo enhancement of dihydromyricetin
Yimei Zheng, Boyu Chen, Xuanxiang Huang, Xiamei Tao, Chao Ai, Yanan Zhao, Peng Liang, Lei Chen
Abstract
• Solubility and stability efficacy of dihydromyricetin (DYM) were improved by SMEDDS. • SMEDDS significantly increased the in vitro release of DYM. • SMEDDS showed superiority in delivering DYM. • DYM-SMEDDS exhibited superior anti-inflammatory and hepatoprotective effects. To enhance the stability and anti-inflammatory efficacy of dihydromyricetin (DYM), suitable excipients were selected for the development of a self-microemulsifying drug delivery system (SMEDDS). The formulated SMEDDS exhibited remarkable drug loading (117.47 ± 4.5 mg/g) and encapsulation rates (93.98 ± 3.6 %). Transmission electron microscope (TEM) revealed the nanoscale and spherical morphology of DYM-SMEDDS. Stability assessments demonstrated that DYM-SMEDDS maintained a consistent uniform small particle size after various cycles of exposure. In vitro release curve exhibited that DYM-SMEDDS released 91.27 ± 1.44 % of DYM within 24 h, surpassing the suspension by 2-fold. Furthermore, in vivo studies indicated that DYM-SMEDDS significantly inhibited the levels of pro-inflammatory factors, while promoting the activity of antioxidant enzymes (p < 0.05). These findings underscore the preventive effects of DYM-SMEDDS against inflammation induced by lipopolysaccharide in mice. In conclusion, SMEDDS exhibits promising potential for oral administration, providing an effective platform for enhancing the efficacy of poorly soluble flavonoids.