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| Formulation optimization and characterization of self-microemulsifying system for dihydromyricetin |
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| DOI：10.19902/j.cnki.zgyz.1003-7969.240080 |
| KeyWord:dihydromyricetin self-microemulsion simplex lattice method in vitro release |
| FundProject:国家自然科学基金项目（32272446）；陕西省科技厅重点研发计划项目（2022NY-223）；陕西省西安市科技局农业技术研发计划项目（21NYYF0058）；陕西省重点研发计划项目（2023-YBSF-379） |
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| Abstract: |
| In order to improve the bioavailability of dihydromyricetin (DMY), dihydromyricetin self-microemulsifying system (DMY-SMES) was prepared. The solubility of DMY in excipients (oil phase, emulsifier, and co-emulsifier) and the compatibility of each excipient were investigated to determine the oil phase, emulsifier, and co-emulsifier. The proportions of these components in the self-microemulsifying system were determined based on the pseudo-ternary phase diagram. Then, the formulation of DMY-SMES was optimized by the simplex lattice method using particle size, polydispersity index (PDI) and drug loading as indicators. The DMY-SMES prepared with the optimal formulation was characterized. The results showed that with medium-chain triglycerides (MCT), Tween-80, and polyethylene glycol 400 as oil phase, emulsifier and co-emulsifier, respectively, the optimal formulation of DMY-SMES was 10% MCT, 60% Tween-80, and 30% polyethylene glycol 400. Under these conditions, the average particle size of DMY-SMES was 14.46 nm, the PDI was 0.138, and the drug loading was 29.84 mg/g, with an encapsulation efficiency of 85.26%. The DMY-SMES obtained from the optimal formulation was a light yellow, clear liquid with spherical-like droplets, small particle size, smooth surface, and no aggregation, forming an O/W type. Both the self-microemulsifying system and its diluted solutions exhibited excellent stability. The cloud point of DMY-SMES was 70 ℃. The particle size and distribution of DMY-SMES in water, pH 1.2 HCl, and pH 6.8 phosphate buffer solution (PBS) showed no significant changes during the 30 d storage period (4 ℃). The release amount of DMY-SMES in water, pH 1.2 HCl, and pH 6.8 PBS was significantly higher than that of free DMY. At a certain mass concentration, the DPPH and ABTS free radical scavenging abilities of DMY-SMES were stronger than those of free DMY. In conclusion, the self-microemulsion system can improve the solubility of DMY, giving DMY good biocompatibility and stability, and it has broad prospects for development in the food industry and pharmaceutical field. |
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