The Preparation Of Illicium Henryi Liposome Cataplasm

The Illicium henryi is the dry root or stem bark of the Illicium of our country.As a Chinese herbal medicine,Illicium henryi has a long history in the civil application,which has effect for promoting Blood circulation to relieve pain and dispelling wind and dampness.The injection of its extraction is widely used in clinic because of its significant effect.However,due to the need for point-injection,the doctor's skill must be high,and the injection may easy to cause adverse reactions during injection and other shortcomings because of its complex composition,which limits the spread of drugs.Therefore,looking for a simple operation,economic security,good patient compliance with Illicium henryi pharmaceutical preparations stared us in the face.Liposomes as a novel drug carrier with similar lipid to sebum,can increase the local concentration of drug in the skin,strengthen the curative effect of local lesions.Drug encapsulated liposomes can accumulate in the corneum and dermis,thus,the drug can be released slowly,lead to a long time directly play on the efficacy of the lesion.However,because of the low viscosity of liposomes that does not have sufficient contact time to skin.As a representative of transdermal drug delivery system,gel plaste(cataplasmata)has many advantages including high loading,adhesion and moisture resistance,aging resistance,no irritation,allergic,no organic solvent pollution.Therefore,in this paper,Illicium henryi was prepared into liposomal cataplasm,in order to obtain a new product of Illicium henryi preparation.In this paper,the content determination method of drug was studied.According to the content of flavonoids of quercetin was determined by high performance liquid chromatography and ultraviolet spectrophotometry.Meanwhile,to study the extraction of effective components of Illicium henryi,three extraction methods ethanol soaking?ethanol reflux extraction and ultrasonic extraction were compared.According to the results,the highest rate is ethanol soaking(4.32%),but there was no significant difference between the three.Next,the formulation and optimization of the liposomes were studied.Through the study of entrapment efficiency of liposomes,the ultrafiltration centrifugation method was used as the determination method.By comparison the entrapment efficiency of liposomes prepared by three methods of ethanol injection,reverse phase evaporation,and membrane dispersion,it is finally determined to use membrane dispersion method for testing.After single factor investigation,the hydration temperature?hydration time and ratio of drug to lipid were studied through orthogonal design.And the best prescription was achieved as the ratio of drug to lipid 1:10;the ratio of cholesterol to phosphorus 1:2;hydration temperature 40 ?,and hydration time 30min.The entrapment efficiency of the liposomes was 81.73%.Then,the optimization of liposome cataplasm formulation was studied.The evaluation index containing cohesive force?permanent adhesion?temperciance?peel strength and appearance evaluation was established on the basis of the 2015 edition of?Chinese Pharmacopoeia?of plaster quality standard,After that,the effects of each substrate on the cataplasm were investigated.Box-Behnken were used to analyze the influence of sodium polyacrylate?polyvinyl pyrrolido?dihydroxyaluminium aminoacetate?glycerine,and the formula was obtained.Finally,the transdermal penetration test of the Illicium henryi liposome cataplasm and the Illicium henryi common cataplasm according to the formula were carried out.The cumulative permeation and skin retention were compared between the two groups.The results showed that the presence of the drug was not detected in both two transdermal receiving solutions in the first six hours due to the presence of the delayed phenomenon of the transdermal formulation.After 8h,the ordinary cataplasm began to release,the release of liposomal cataplasm was slightly later than that of ordinary cataplasm,but the cumulative permeation of liposomal cataplasm was 18.01±1.94?g/cm2 in 72h,which is higher than the cumulative permeation of ordinary cataplasm(7.76 ±1.42?g/cm2).And in the determination of skin retention,it was found that the skin retention of the liposomal cataplasm(5.40 ± 0.22?g/cm2)was higher than that of the ordinary cataplasm(3.11 ±1.18?g/cm2).