Preparation And Quality Evaluation Of Cmcumin Derivative Ethosome

Curcumin?CM?is a plant polyphenol extracted from turmeric,and it is also the most important active ingredient of turmeric for its pharmacological action.In recent years,studies have shown that curcumin has a good role in anti-cancer,anti-inflammatory,anti-oxidation,lipid-lowering,anti-atherosclerosis and other aspects.Literature studies show that curcumin after structural transformation and modification,its biological activity increased,water solubility increased.In this topic,curcumin derivatives?CMD?were prepared into ethosome.A preliminary study of the in vitro and in vivo characteristics of curcumin derivative ethosome?CMDES?was applied to oral drug delivery systems in order to improve poor absorption of poorly soluble drugs,short half-life,and low bioavailability.The main work of this article involves the following sections:An in vitro high performance liquid chromatography?HPLC?method for the determination of CMD in CMDES was established.The specificity,linearity,minimum detection limit,limit of quantitation,precision,recovery,and sample stability of the method were investigated.The results showed that the HPLC method had good specificity,high precision,high recovery,and met the measurement requirements.This method can be used to determine the content of CMD.Hydrophilic adjuvant HA-g-mPEG was synthesized,CMDES was prepared,and the physicochemical properties of CMDES such as morphology,particle size distribution,Zeta potential,encapsulation efficiency,pH and conductivity were investigated.The CMDES was spherical,uniform in size,average particle size?291.80±3.16?nm,Zeta potential?15.3±0.32?mV,and average entrapment efficiency?80.55±1.42?%.The SD rats were orally administered by gavage and the pharmacokinetic characteristics of the rats were investigated.The results showed that the pharmacokinetics of CMDES changed significantly compared with CMD.The AUC?0-72h?for CMD and CMDES was?147.35±12.66??g/L·h and?1503.73±28.69??g/L·h,respectively,and the AUC?0-72h?for CMDES was increased by 9.57 times;The MRT of CMD and CMDES were?2.39±0.86?h and?10.89±1.32?h,respectively.The MRT of CMDES was 4.56 times that of CMD;the Cl of CMD and CMDES were?672.38±107.16?L·h^-1·kg^-1 and?64.07±4.76?L·h^-1·kg^-1,Cl of CMDES is one-tenth of CMD.It showed that the residence time of CMDES in vivo was prolonged,the elimination rate was lower than that of CM,and the bioavailability of CMDES was significantly improved.