Preparation Of Berberine Hydrochloride Liposomes-geland Its Preliminary Pharmacodynamic Evaluation On Eczema

Objective:In this paper,liposomes-gel was designed for the delivery of berberine hydrochloride on the skin.The quality of liposomes-gel was evaluated.To study the release characteristics in vitro and antioxidant activity of berberine hydrochloride liposomes-gel and its therapeutic effect on eczema,so as to provide some reference for the treatment and application of berberine hydrochloride in skin diseases.Methods:Liposomes were prepared from soybean lecithin and cholesterol,and the appropriate preparation method was selected according to the encapsulation efficiency.Sodium alginate was added to the prepared liposomes to make liposomes-gel by natural swelling,and its morphology,viscosity,pH and release kinetics in vitro were investigated.The antioxidant capacity of berberine hydrochloride liposomes-gel was evaluated by scavenging DPPH free radicals and H2O2 and inhibiting lipid peroxide MDA.The model of eczema was established,and the curative effect of eczema was evaluated by ear swelling,spleen index and pathological section.Results:According to the results of encapsulation efficiency,liposomes was prepared by the film dispersion method.The prepared liposomes were spherical,uniform in size,with encapsulation efficiency of 79.69±4.5%and particle size of 153.7±11.2 nm,and the encapsulation efficiency and particle size were stable after storage at 4℃ for 30 days.Berberine hydrochloride liposomes-gel has fine texture and uniform dispersion,and its viscosity and pH are 17.98±7.57 mPas and 7.33±0.07 respectively.It showed a good sustained-release effect in the study of release rate in vitro,and the release curve conformed to Higuchi model.The cumulative release rate per unit area of transdermal delivery was 85.01±4.53(ig/cm2,which provided ideas for the application and treatment of skin diseases.The IC50 of berberine hydrochloride to DPPH radical is 2.22 mg/mL,and the IC50 to H2O2 is 1.29 mg/mL,and it can effectively inhibit the production of liver lipid peroxide MDA in the concentration range of 0.4～2.0 mg/mL.Soybean phospholipid has a good scavenging ability for DPPH and H2O2,and its good antioxidant ability also endows the prepared liposomes with antioxidant properties.The antioxidant activity of berberine hydrochloride liposomes-gel lays a foundation for further study on its therapeutic effect on eczema.2,4-dinitrochlorobenzene sensitized mouse eczema model was established.Berberine hydrochloride and its preparation were used for local skin administration.After 12 days of administration,it was found that berberine hydrochloride liposomesgel could reduce ear swelling and spleen index caused by eczema,and had good antiinflammatory effect,and could alleviate itching caused by eczema.Skin tissue section can be observed that the drug can reduce the epidermal thickening,cell edema and inflammatory cell infiltration caused by eczema.Conclusion:Berberine hydrochloride liposomes-gel has good skin permeability and good sustained-release effect,and is suitable for skin administration.At the same time,berberine hydrochloride liposomes-gel has good antioxidant capacity.Preliminary pharmacodynamic experiments show that berberine hydrochloride liposomes-gel can effectively alleviate itching,inflammation and allergic symptoms caused by eczema,and provide a new strategy for clinical application and treatment of eczema.