Preparation Of Optimized Curcumin Nanoliposomes And Study Its Characteristics In Vitro And In Vivo

Curcumin(Cur)is an orange-yellow crystalline polyphenols extracted from the rhizome of turmeric.It is generally considered to be the most effective component of turmeric.It has many pharmacological effects such as anti-oxidation,anti-diabetic nephropathy,hypoglycemia,prevention and treatment of thrombosis,especially anti-tumor activity.Curcumin has fewer adverse reactions and abundant resources,which make it has better utilize.Curcumin has poor solubility and low bio availability,which limits the clinical application of curcumin.In order to improve the solubility of curcumin and to meet the administration conditions,the researchers have developed a variety of curcumin drug delivery systems.For example,liposomes,polymer nanoparticles,adhesives,lipid nanoparticles,etc.As one of superior drug carriers,liposomes have excellent characteristics of improving drug solubility,enhancing drug target and stability.In recent years,the study of curcumin liposomes is mainly focused on optimizing the preparation process,in order to improve the drug loading of liposomes,and thus to meet the treatment of drug delivery conditions to improve the anti-cancer effect.The purpose of this study was to prepare curcumin nanoliposomes(cur-np)with suitable size,stable structure and high entrapment efficiency.This topic is divided into two parts:1.Preparation of cur-np and study the properties of cur-np in vitroOptimize the preparation process of cur-np,in order to improve the encapsulation efficiency and stability of cur-np.At the same time,the proliferation effects of the cur-np on Hep G2 cells?SMMC-7721 cells?Bel-7402 cells and SGC-7901 cells were explored.With the indexes of encapsulation efficiency and particle size,formulation process of cur-np was optimized by orthogonal design.In vitro experiments were performed to determine the inhibitory effect of curcumin and cur-np on Hep G2 cells?SMMC-7721 cells ? Bel-7402 cells and SGC-7901 cells by MTT assay.The encapsulation efficiency of cur-np was(11.64±1.35)%.The particle size of cur-np was(114.57±18.57)nm and zeta potential was(-8.76±0.38)m V.The optimized prescription of the cur-np has high encapsulation efficiency and sustained release properties.cur-np has a good inhibitory effect on tumor,and the effect depends on dose and time.This study provided theoretical guides for the further application of curcumin liposomes.2.In vivo pharmacokinetic study of cur-npThe accurate and precise detection method is established by HPLC,which has the advantages of simple operation,fast determination and easy reagent availability.After curcumin and cur-np solution were administered via the tail vein,the pharmacokinetics of curcumin in rats was analyzed.The clearance rate(Clz)of free curcumin and cur-np was 0.22±0.05 and 0.14±0.02,respectively,indicated that compared with free curcumin,cur-np eliminated slower and resided a long time in vivo.The pharmacokinetics provided a reference for the further research of curcumin liposomes.