Study On Harmine Hydrochloride Transfersomes Transdermal Drug Delivery System And Niosomes Transdermal Drug Delivery System

Objective: To optimize the prescriptions of harmine hydrochloride (HM·HCl)transfersomes creams and niosomes creams, evaluate the transdermal absorption and theeffect of anti-psoriasis. Methods:1) The models with vagina epithelium mitosis and theformation of granular layer in scale epidermis of mice tails were used to investigate thetherapeutic effects of HM·HCl and total alkaloids from P. harmala. The dose-effectrelationship of HM·HCl was studied.2) The recovery rate was selected as index, a suiTab.method was found which was used to evaluate the entrapment efficiency of transfersomesand niosomes.3) Uniform design was used for selecting the technology condition ofHM·HCl transfersomes and niosomes with the encapsulation efficiency as index.4)According to the entrapment efficiency, particle size and zeta potential, the kinds andconcentration of cryoprotectants for transfersomes and niosomes were selected.5) Acomprehensive score system was established as optimization index. The uniform designwere used for selecting the prescription of HM·HCl transfersomes and niosomes creams.6)According to the accumulated permeation amount(Q) and intracutaneous drug retentionamount, the transdermal effect of the HM·HCl transfersomes cream, the transdermalabsorption of HM·HCl niosomes cream and HM·HCl cream were evaluated respectively.7)The anti-psoriasis effect of HM·HCl transfersomes cream and niosomes cream wereinvestigated.Results:1) The results indicated that HM·HCl and total alkaloids from P. harmala couldsignificantly inhibit vagina epithelium mitosis, and promote the formation of granularlayer in scale epidermis of mice tails. According to the results of vagina epithelium mitosisinhibition, the effect of HM·HCl was better than that of total alkaloids from P. harmala (P ﹤0.01). HM·HCl showed obviously dose-dependent effects on the two models animals.2)The sephadex column chromatography was used to separate the free drug andtransfersomes or niosomes, and the eluant was deionized water. The average recovery rateof transfersomes and niosomes were98.72%and98.59%respectively.3) The filmdispersion method was selected to prepare HM·HCl transfersomes, the averageencapsulation efficiency was88.02%. The reverse evaporation method was chosen toprepare HM·HCl niosomes, the average encapsulation efficiency was81.15%.4)15%mannitol was the suiTab. cryoprotectant for HM·HCl transfersomes, and15%sucrose wasthe suiTab. cryoprotectant for HM·HCl niosomes.5) The optimized formula of HM·HCltransfersomes cream was as follows: monostearin8%, vaseline5%, liquid paraffin6.1%,Span-801.9%, Tween-803.8%, sodium dodecylsulphate (SDS)0.8%. The optimizedformula of HM·HCl niosomes cream was as follows: monostearin8%, vaseline5%, liquidparaffin6.1%, Span-801.1%, Tween-802.2%; sodium dodecyl sulphate (SDS)0.8%.6)The accumulated permeation amount(Q) of HM·HCl in transfersomes and niosomescreams were200.19μg·cm-2,27.53μg·cm-2respectively. The intracutaneous drug retentionof HM·HCl in transfersomes and niosomes creams were891.23μg g-1,616.87μg g-1respectively.7) Both HM·HCl transfersomes and niosomes creams could significantlyinhibit vagina epithelium mitosis, and promote the formation of granular layer in scaleepidermis of mice tails. Conclusion: The prescription of HM·HCl transfersomes andniosomes creams were available, reasonable, and reproducible. HM·HCl transfersomesand niosomes creams both exhibited beneficial therapeutic effects on mice model ofpsoriasis.