| Baicalin was one of the main active ingredients of Scutellaria baicalensis.It had various effects such as detoxification,antibacterial,anti-inflammatory,liver protection,anti-oxidation,anti-thrombosis,anti-fungal and anti-tumor.The presently available baicalin formulation were baicalin tablets and baicalin capsules for the treatment of acute and chronic hepatitis.Baicalin was insoluble in water and lipids,what's more,it was unstable under alkaline conditions.Aimed at the physicochemical properties of baicalin,this paper synthesized a variety of experimental design methods to prepare baicalin microemulsion gel,and its preliminary pharmacodynamic was studied,further,its skin compatibility was investigated,with a view to baicalin development become a local new percutaneous medicine lay the experimental foundation.In this study,the formulation of baicalin microemulsion was determined by the equilibrium solubility and the pseudo-ternary phase diagram method;the ratio of baicalin microemulsion formulation was optimized by the central composite design method and the Franz diffusion cell method in order to select the small size.,high drug loading,good transdermal properties of baicalin microemulsion prescription.The final prescriptions were:Ethyl oleate 4.48%,Tween 80 31.64%,Glycerol 13.88%,pH7.4 phosphate buffer 50%,the drug content was?1.03±0.04?%,and the entrapment efficiency was?95.28±3.17?%,average particle size was?15.95±0.77?nm,PDI was?0.131±0.058?,Zeta potential was-32.4 mv,pH was 5.67,and the stability of baicalin microemulsion was good.In this study,split plot design method was used.Using the transdermal performance as an index,the amount of the gel matrix and the amount and type of the transdermal enhancer were simultaneously examined to select the appropriate composition of the baicalin microemulsion gel.The results showed that the best prescription was:0.5%xanthan gum or 1.5%carboxymethylcellulose sodium as the gel matrix,2%borneol and0.5%clove oil as the penetration enhancer,and the rest was baicalin microemulsion.Taking xanthan microemulsion gel as an example,its particle size is?15.71±0.41?nm,its pH is?5.95±0.10?,its drug loading is?10.42±0.08?mg/g,and its encapsulation efficiency is?97.17±2.70?%.When observed in atomic force microscopy and transmission electron microscopy,the baicalin microemulsion gel particles are round-like,well dispersed and uniform in particle size.In Franz diffusion cell test,cumulative penetration amounts of baicalin microemulsion gel within 12 h was?672.14±44.11??g·cm-2.In this study,the anti-inflammatory and analgesic effects of baicalin microemulsion gel were investigated by xylene-induced mouse ear edema model,acetic acid writhing test model and hot plat induced injury model.Compared to the blank group,baicalin microemulsion gel showed significant anti-inflammatory and analgesic effects.At the same time,by comparing the growth rate,the skin condition and pathological section results,it was found that the baicalin microemulsion gel had no effect on the growth of the mice,had was safer than positive drug?Compound Dexamethasone and Riftaline Emulsion?.In summary,baicalin microemulsion gel has the advantages of simple preparation process,small particle,uniform distribution,high safety,significant anti-inflammatory and analgesic effects,developing it a good clinical application prospect. |
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