The Preparation And Property Of Periplaneta Americana Extract Liposome For Skin Repair

The skin is the largest organ of the human body that covers the surface of the human body and plays a protective role.However,skin trauma can occur due to various reasons.At present,the main active substances of some drugs used in wound repair are polar macromolecules soluble in water,which are not easy to reach the lesion site through the surface of the skin.Its efficacy and practical application are limited to a certain extent.Liposome(LIP)has biofilm with a bilayer structure similar to the human cell membrane,which has a similar structure and better biocompatibility to the stratum corneum than the other drug carriers,It can be well absorbed by the stratum corneum when it wraps the drug,and forms a drug reservoir between the epidermis and the dermis,so as to achieve the purpose of continuous release of the drug and improve the therapeutic effect.This paper studies the preparation of Periplaneta Americana extract liposome(PAE-LIP),discusses the effects of process conditions and component formulations on the encapsulation efficiency,and further makes drug-loaded liposomes into gel preparation The skin permeability and anti-inflammatory properties of the gel formulation were characterized.The main research contents are as follows:(1)Using ethanol injection method,with ethanol as the organic phase and the Periplaneta americana extract solution as the aqueous phase,Periplaneta Americana extract liposome(PAE-LIP)was prepared.By designing orthogonal experiments,the effect of the temperature(T),stirring intensity,concentration of lecithin(EPC),the mass ratio of lecithin to cholesterol(mEPC:mCHO),the ratio of aqueous phase to organic phase(Qa:Qw)on the encapsulation efficiency of Periplaneta americana extract liposomes was investigated.The optimum process conditions are as follow:temperature:40?,stirring intensity:750 r/min,lecithin concentration:45 mg/mL,the mass ratio of lecithin to cholesterol:7.5:1,the ratio of aqueous phase to organic phase:1:1,the encapsulation efficiency is 41.6%.Further,the Periplaneta American extract ultradeformable liposome(PAE-ULIP)was prepared to enhance the deformability of the liposome and improve the skin permeability.By comparing the HLB values and related properties of different surfactants,Tween-20 was selected as the softener,and the effect of the amount of Tween-20 on the encapsulation efficiency was investigated.The dosage of Tween-20 under high encapsulation efficiency is:the mass ratio of Tween-20 to EPC is 1:10,and the encapsulation efficiency is 46.2%;(2)PAE gel,PAE-LIP gel,and PAE-ULIP gel were prepared.First of all,the in vitro release performance of these three gels were characterized.The cumulative drug release rates of the three gels in 24 h are 60.4%,52.1%,and 61.8%,respectively;The in vitro transdermal properties of the three gels were measured,and the cumulative release amount per unit area of PAE-ULIP gel in 24 hour was(690 � 38)?g/cm2,the cumulative release amount per unit area of PAE-LIP gel in 24 hour is(550�36)?g/cm2,and the PAE gel almost failed to penetrate the Strat-M membrane.The results show that the liposome gel significantly enhanced the transdermal permeability of the drug,and the ultradeformable liposome gel has better skin permeability.(3)The anti-inflammatory activity of PAE-ULIP gel was detected by enzyme-linked immunosorbent assay,and the anti-inflammatory property of the drug was characterized by measuring the concentration of inflammatory factor TNF-? in cell culture medium.The concentration of TNF-? in the cell supernatant was 1181.6 ng/mL without adding drugs.After adding PAE solution and PAE-ULIP gel,the concentration of TNF-? in the supernatants was 667.7 ng/mL and 862.6 ng/mL respectively,and the release of inflammatory factors was inhibited.After the stimulation of lipopolysaccharide(LPS),the concentration of TNF-? in the supernatant was 1529.3 ng/mL,and after adding the two forms of drugs respectively,the concentrations of TNF-? in the supernatant were 1153.6ng/mL and 1095.9ng/mL,respectively.The release of inflammatory factors was also inhibited.It shows that the PAE-ULIP gel form in this study has no significant effect on the anti-inflammatory activity of the active components of PAE,but also has anti-inflammatory activity.