ABSTRACT
AIM: To prepare radix scutellariae microemulsion gel and investigate its therapeutic effect on chronic eczema based on the previous research of radix scutellariae self microemulsion. METHODS: The gel matrix and humectant were optimized by single factor method and response surface method to obtain the formula and preparation technique of the gel. The Franz diffusion cell method was used to evaluate the transdermal properties of microemulsion and microemulsion gel in vitro. By establishing a chronic eczema model in the mouse ear, the swelling degree, swelling inhibition rate, pathological changes and tumor necrosis factor α (TNF-α), Interleukin-1β (IL-1β) and interleukin - 6 (IL-6) of radix scutellariae microemulsion gel were measured, to investigate the therapeutic effect on chronic eczema in mice. RESULTS: The physical and chemical properties of radix scutellariae microemulsion gel were stable. Compared with microemulsion, the microemulsion gel had better transdermal performance. The cumulative transdermal amount of baicalein and wogonin, the main components of microemulsion gel, was 1.85 times and 2.77 times of that of microemulsion respectively. Moreover, the steady flow rate and permeability coefficient of microemulsion gel significantly increased, and the lag time significantly shortened. Pharmacodynamic study showed that compared with the model group, the radix scutellariae microemulsion gel could significantly reduce the ear swelling of mice (P<0.05), and the serum inflammatory factor TNF - α, IL-1β and IL-6 reduced content by over 37%. Compared with the radix scutellaria aqueous extract and aqueous extract gel, the treatment of chronic eczema was better. CONCLUSION: The preparation process of radix scutellaria microemulsion gel is feasible, with strong transdermal property, and a significant therapeutic effect on chronic eczema.
ABSTRACT
Western blotting of autophagic markers LC3Ⅱ and p62 are widely used for estimating autophagic activity. To compare the regulation of various autophagy modulators on LC3Ⅱ and p62,HEK293 cells were treated separately with mTOR-dependent autophagy activator rapamycin or -independent autophagy activators trehalose, and autophagy inhibitors including 3-methyladenine (3-MA),bafilomycin A1 or E64d and pepstatin A that inhi-bited the initiation of autophagy,the fusion of autophagosome and lysosome,and the activities of lysosomal enzymes accordingly,and then LC3Ⅱ and p62 levels were assessed. Western blot results demonstrated that rapam-ycin enhanced the conversion of LC3I to LC3Ⅱ,promoted the degradation of p62 simultaneously,while trehalose merely increased the expression of LC3Ⅱ with no influence on the p62 level. Moreover,inhibition of autophagy commonly led to accumulation of LC3Ⅱ as well as blockage of p62 degradation in a concentration- and time-dependent manner. These results indicate that obvious differences exist in the regulation of LC3Ⅱ and p62 by various modulators although both are autophagic markers.