The Research On Preparation Of EGCG-Vardenafil Nanoparticles And Its Antitumor Effect

With the rapid development of society,environmental pollution,the diversity of materials structure,irregular diet and other factors led to the increasing incidence of cancer diseases,cancer has become one of the most diseases that endanger human health.At the same time,the cost of treatment of cancerous diseases,especially malignancies,is increasing year by year,which cause patient's serious physical pain,but also to the caused and serious family burden.EGCG as an important biological component in green tea possesses anticancer,prevention of cardiovascular disease,and improvement of immune system.However,it has been found that EGCG has a low bioavailability and is particularly susceptible to oxidation due to light and temperature.In this study,we aim to prepare EGCG formulation of nanoparticles to improve the effectiveness against cancers by co-assembling of EGCG and?-lactoglobulin with the presence of vardenafil.The main work include the preparation of EGCG-?-lactoglobulin nanoparticles,the optimization of vardenafil amount in the nanoparticles,and the effectiveness of the nanoparticles agaist tumors.The details are as follows:(1)The effect of vardenafil in EGCG-?-lactoglobulin nanoparticles was studied.The experimental results show that EGCG/?-lactoglobulin at a the rate of 1:4(w/w)could significantly improve the stability of EGCG-?-lactoglobulin nanoparticles(E?-NPs),and a addition of vardenafil in the EGCG-?-lactoglobulin nanoparticles could change the size and stability of nanoparticles.When EGCG and vardenafil at aratio of 5:1,EGCG-vardenafil-?-lactoglobulin nanoparticles(EV?-NPs)gave nanoparticles with size of73 nm,which showed good stability and significantly enhanced proliferative inhibition against cancer cells A375 and HGC-27,compared to EGCG and E?-NPs.(2)The effect of EV?-NPs on cancer cells was studied by using iodide iodination staining(PI)determination and Annexin-V staining to determine DNA damage,cell cycle arrest,and apoptosis and necrosis.The experimental results showed EV?-NPs promoted the apoptosis of A375 cells since it could lead to significant cell cycle arrest in S phase,obvious nuclear division,up-regulation of the expression of Caspase-9 and Caspase-3.(3)The inhibitory effect of EV?-NPs on tumor growth in vivo was studied.The results showed that the antitumor effect of EV?-NPs was significantly higher than that of E?-NPs.The weight of liver and spleen of the mice were not significantly affected by the EV?-NPs at the end of the trial,indicating that EV?-NPs had no obvious toxicity.The results of this study can provide a scientific basis for the development of new anti-tumor products of EGCG.