Preparation And Study Of The Podophyllotoxin DPPC Proliposome

Objective:Condyloma acuminatum(CA) is a kind of sexually transmitted disease(STDs), with the progressive incidence,it is now in the second place of STDs. Which is human papillomavirus(HPV), a kind of virus, that leads to CA. This kind of virus live autoeciously in the nucleolus of basal cells,while a few of them in the outside of the cells. HPV inside is the main source of relapse and can exist latently in a long period. 0.5% podophyllotoxin tincture is an effective drug advocated by WHO.Podophyllotoxin can be used to treat CA for it has the effect of restraining the division growth process of these cells infected by HPV,and leading putrescence and amotic of these cells.Podophyllotoxin is recommended by WHO as valid for CA,and 0.5% podophyllotoxin tincture is commonly used in treatment.However,0.5% podophyllotoxin tincture can only be used to the warts that can be seen with eyes, and if it is used extensive,serious side-effects will take place. Liposome is the neotype carrier that can controll and delay release of drug from the proparation, which has been studied by many scientist in recent years.Making PPT into Liposome can improve its curative effect of anti-relapse of CA by ameliorating its Pharmacokinetics and pharmacodynamics to the certain degree.As literature described, that better effects can be achieved when some drug is incapsuled in DPPC liposome for skin use. But general Liposome is inadequate tranquilization for liquid Liposome medicine have the matter of getting together of particle,and oxidize and decomposition of the phospholipid,and the leakage of the medicine enveloped in Liposome,etc.Proliposome is a solid praeparatum and the dehydration format of the liposome ingredient and the protectant for protectant.lt can re-establish into liposome inmedium. Proliposome can solve the matter of oxidizing, hydrolysis, aggregation, delamination, seepaging of medicine,and pyro-degerming,etc.which can conquer the problem of stability when the liquid liposome be long-term deposited.And it is the key of the industrialization and the commercialization of the liposome. Based on the related literature and appropriate medical formula sifted in advance, PPT-DPPC-PL was prepared. The animal experiment and the primary clinical trial was carried out.Methods: Reverse-phase evaporation vesicles (REV) method was used to prepare PPT-DPPC liposomes(ordinary PPT-DPPC liposomes). Freeze-drying method was used to prepare PPT-DPPC proliposomes(PPT-DPPC-PL).The particle morphology, the size range, the encapsulation efficiency and the stability of PPT-DPPC liposomes were investigated.The PPT-DPPC-PL's stability was studied by mensurating its grain size in water under four kinds of different intension physics outside force. The proliposomes were stored at 4 ~40 for 1~6 months remained. The particle morphology, the size range, the encapsulation efficiency and the stability of PPT-DPPC liposomes were investigated after PPT-DPPC-PL was stored at 4~40 for 1-6 months and was hydrated.2 Ten porkets were chosed and separated into 2 groups,then 2 two kinds of podophyllotoxin liposome were applied on the skin. The porkets' blood were sampled and drug concentrations were examined at different time.3 PPT-DPPC-PL was used to treat the patients suffering from CA.And the primary clinical effect of the preparations volunteers was observed.Results:1 The PPT-DPPC-PL is a loosen and lily powder. The form of thePPT-DPPC-PL after hydrated isn't different from the form of the ordinary PPT-DPPC-L.After PPT-DPPC-PL was hydrated , PPT-DPPC liposomes appeared multivesicular under electron microscope. The particle were distributed homogenously. The average particle size was 1.45+0.38 H m.The encapsulation efficiency of PPT was 72.3%.The proliposomes were stored at 4~40 for 1-6 months and were stable.2 In our experiments, the podophyllotoxin of two kinds of PPT-DPPC-L concentrations in animals' blood were no difference. The trend of the podophyllotoxin of two kinds of PPT-DPPC-L concentrations in animals' blood were no difference..3...