Optimization Of The Preparation Process Of EGCG Loaded FA-conjugated BSA Nanopartides For Tumor-targeted Drug Delivery Using Factorial Design

Catechin is the main polyphenol in tea, it has many advantages such as anti-oxidation, antip-hlogosis, antip-radiation and control tumor cells. Epigallocatechin-3-gallate (EGCG) is the main function of Catechins in the active material. EGCG accounts for 45% to 65% in the total catechins in Catechins. Therefore, EGCG is the most abundant in green tea, the nature's most active catechins. EGCG's antioxidant activity is 20 times than vitamin E and 6 times than peroxide dismutase (SOD).EGCG has obvious harmacological effect on ridding free, controlling tumor cells, anti-inflammatory, anti-mutation, anti-aging and improving liver function and so on. It has already became the focal point on caffeine separation, the purification and the clinical practice research. But at present it is difficulte to use high dose's EGCG injection get the highly effective control on restrained the tumour cell growth and the shift, these serious influence need clinical care effect.Targeting drug delivery system (TDDS) is a kind of new medicinethe craft, It can transport the medicine to the target organ with maximum limit, but has very small influence to the non-target organ to achieves the highly effective and low poisonous treatment result, especially is suitable in treating cancers. The targeted medicine can carry on the the targeting drug delivery system, and can direct the medicine delivery to the medicine goal spot. it may cause the medicine dose,which needs to arrive the medicine spot increase greatly to reduces the use dose and the medicine the poisonous side effect. In recent years, how to enhance the anticancer treatment medicine local concentration, cancer cell's selectivity and whole body's poisonous side reaction aspect get distinct progress. At present, the research of kinds of target-drug carrier already make a big progress, developing the target medicine is a current pharmacy important domain.Nanoparticles is a kind of widely applied carrier for the nontoxicity, solubility and high biological exploitability, in medicine clinical research aspects and pharmacology research. The albumin nanoparticles carrier is composed of the albumin, which has formed the solid spheroid after the solidification separation can adsorb or bundle the medicine. The albumin carrier has many advantages, It can reduce the medicine release's time, enhances the medicine stability not to decompose in the vivo and it also has the advantages of the non-toxic side effect and the immune response. Therefore the research of albumin nanoparticles carrier also get more and more thoroughly.This article is mainly based on the EGCG anti-tumor effectiveness, use Nano technology and Targeted technical to prepare the EGCG loaded FA-conjugated BSA nanoparticles (FA-EGCG-BSANP).We has carried on the multi-influencing factor experiment through two factor design software, and obtained a nanometer target preparation most superior result. Use HPLC and Laser Particle Size Analyzer to carry on the examination of an optimized nanometer medicine, examined the medicine appearance characteristic and the medicine content.The topic research conclusion obtains:1,Obtains the primary influence factor of nanometer medicine particle size, the envelope rate and carries the dose by two level experimental design. Makes the adjustment to the different influencing factor to obtain the optimized result.2,Examines through the Laser Particle Size and the scanning electron microscope obtains the particle size is about 170nm, the shape is close for the sphere arrangement.3,Use HPLC obtains a nanometer medicine drug entrapment efficiency (DEE) and drug-loading efficiency (DLE) and the obtained result is that drug entrapment efficiency is (84.6±0.5)%,drug-loading efficiency is (29.9±0.6)%4,Use the ultraviolet spectrophotometric method carries on the scanning, the FA conjugated percentage and the albumin coupling quantity, the result is, the FA coupling quantity is 18.363μg·mg-1BSA.5,Obtained the drug release data through the examination in phosphoric acid buffer solution release and the test result had demonstrated EGCG released situation in 24 hours from the medicine.Through the above examination we can obtain the best optimized condition of prepares FA-EGCG-BSANP. We can also accurately examine its appearance characteristic, drug entrapment efficiency, drug-loading efficiency and drug release. Provide important evidence to further study of medicine provides in vivo active metabolism and target tropism on EGCG.