Study On The Liposomes And Ethosomes Of Doliroside B

With the accelerated pace of human life,people work under great pressure and eating habits have changed dramatically.Consequently,the incidence of gout has increased.Gouty arthritisis the main clinical manifestation,due to the excessive amount of uric acid in the body,which can’t be excreted successfully.The deposition of uric acid in articular cartilage,joint capsule,and other tissues causes joint swelling,fever and pain.Currently,more and more people are suffering from the disease,which greatly disturbs the person’s daily life.Doliroside B is one of the main active ingredients of the dolichos.It can significantly reduce inflammatory cytokines at sites of inflammation.This project was aimed to design a reasonable dosage of doliroside B for the treatment of gouty arthritis.The main work is summarized as follows.Firstly,HPLC method has been developed for analyzing the contents of doliroside B in the total saponins from Dolichos appendiculatus Hand.-Mazz.The method is simple and straight forward.The equipment sets are easy to get.In addition,results obtained are accurate with good repeatability.Moreover,the symmetry factor and number of theoretical plates keep in line with Pharmacopoeia.Secondly,the preformulation has been carried out.Physicochemical properties of doliroside B were investigated,including PKa,solubility,and apparent oil-water partition coefficient(Papp).p Ka1 and p Ka2 are 6.86,and 8.1,respectively.And the results show that it was slightly dissolved in these medium.The Papp decreased with the increase of p H in different p H n-octanol / water system and changed greatly between 6.0-6.8,which coincided with the p Ka1.Intestinal perfusion was used to study the absorption of doliroside B in the intestine of rats.The experiments showed that absorption rate was higher in p H=6 than p H=7.4,and that absorption rate was higher in duodenum than total intestinal segment.Third,different methods to determinate the encapsulation efficiency of the liposomes of doliroside B were compared including ultrafiltration 、 high-speed centrifugation、 dextran gel column、dialysis.The results showed that the dialysis was the best.It was simple-operated、low-costed,and had good repeatability.Based the criterion of encapsulation efficiency,the different prescriptions and processes were compared with single factor experiment.The formulation was optimized on the basis of four factors and there levels.The ethosomes of doliroside B was prepared by the injection method.In addition,the liposomes and ethosomes were characterized.The morphology was determined by transmission electron microscope.The particle size was measured by Malvern Zetasizer.The encapsulation efficiency was measured by dialysis.At last,HPLC-ELSD method was established for analyzing the contents of doliroside B in the percutaneous absorption experiment with high accuracy,good reproducibility.This greatly reduced the limit of quantification of doliroside B compared with HPLC-UV.The drug permeability of alcoholic solution,ethosomes and conventional liposomes was investigated,including absorption rate and the cumulative amount.It showed a significant difference.Cd Te QDs was encapsulated into ethosomes and liposomes instead of doliroside B,which made fluorescent to visualize the skin delivery of the tested vesicles.As a result,the retention amount of ethosomes and liposomes in epidermis was greater than in the dermis.The retention amount of ethosomes was greater than liposomes both in epidermis and dermis.