Preparation And Activity And Target Ability Evaluation On Folate-conjugated EGCG Albumin Nanoparticles

Epigallocatechin-3-gallate(EGCG) is extracted from the green tea,it is the one kinds of the tea polyphenols.EGCG has many advantages,for example,widely resouce,non-toxicity and easy to dissolved in the water.With the development of the technology,scientists found that EGCG can control tumor cells,anti-oxidation,antisepsis and antiphlogosis,EGCG is the exploiable natural product.But,EGCG is too weak to attack the tumor cell in vivo,and the biological availability is also very low.At present,high dose EGCG is also difficulty to control tmor cells diffusion.These are all can be influenced the tumor treatment effect.Prostatic cancer is considered one of the widely incidence of a disease,in Occident the death rate of the prostatic cancer second to the lung cancer.In China,the prostatic cancer expand so fast,between the 1950s to 1990s,the incidence of disease increase to 1.2～3.4 per Hundred Thousand.The men who are upward 70 years old,the incidence of the prostatic cancer can reach to 25%.Recenctly,scientists found that drinking green tea everyday can help reduce the probability of the prostatic cancer.Later,scientists make clear that the effective constituent which in the green tea is the EGCG.EGCG can adjust the apoptin proteid,and control the circle of the cancer cells.In all,EGCG can make the cancer cells lose the transfer and diffuse ability.Target technology(TDDS) is a new type technology,it can be transport the remedy to the target organ,and have no influence to the non-target organ.It is comply to the treatment of the tumor.This text combine the advantage of EGCG and the nanotechnology.To study the preparation,activity and target ability evaluation in vitro on epigallocatechin-3-gallate (EGCG) bovine serum albumin nanoparticles targeting to PC-3 cells,the EGCG bovine serum albumin nanoparticles mediated folate(FA-EGCG-BSANP) were prepared by desolvation process.1,The morphology and particle size of the nanoparticles were determined by atomic force microscope(AFM),The morphology and particle size distribution of FA-EGCG-BSANP were uniform and even with the mean particle size of 200 nm;2,HPLC was used to analyse the entrapment efficiency and drug loading rate of EGCG., The drug embedding and loading rate of EGCG were(81.5±1.8)%and(29.3±0.6)%;3,The amount of folate conjugation on the BSANP was determined by quantitative ultraviolet(UV) spectrophotometer analysis,the amount of folate conjugation was 18.363μg·mg^-1BSA;4,The target ability to PC-3 was observed using laser scanning confocal microscope (LSCM) and fluorophotometer microscope.The FA-EGCG-BSANP uptakes by cultured PC-3 cells were 23.65 times the amount of EGCG-BSANP in a concentration dependant manner.The lethality of PC-3 cells treated FA-EGCG-BSA was 82.8%,while EGCG and EGCG-BSANP were 58.6%and 55.1%,respectively.And lethality of PC-3 cells was positively correlation with nanoparticles uptake amount;5,The activity of FA-EGCG-BSANP was mensurated by MTT method.FA-EGCG-BSANP can significantly enhance EGCG to PC-3 cells sites and improve their efficacy,which is considered to an experimental foundation for furth er research on its activity,target ability and metabolism in vivo.