Study On The Preparation And Bioavailability Of Curcumin Micro Pellets And Curcumin Niosomes

Curcumin possesses important biological and pharmacological activities and becomes a potential compound for prevention and treatment of cancer and other diseases.However,curcumin is unstable in alkaline conditions and insoluble in water,which leads to low bioavailability in vivo and limits its use in clinical practice.In this paper,curcumin gastric floating micro pellets and curcumin niosomes were prepared.Gastric floating micro pellets could prolong gastric retention time,improve the therapeutic effect of gastric diseases(gastric cancer,gastritis)and prevent degradation of curcumin in intestinal alkaline site to obtain better bioavailability.Niosomes could improve the solubility,slow down the release of curcumin,and prolong the time of blood circulation.Curcumin niosomes also could be targeted to the liver and spleen,improve the curative effect of liver cancer,hepatitis and other diseases.Curcumin gastric floating micro pellets were prepared by high-speed stirring melt method.With floating time as index,the formulation and technology of curcumin gastric floating micro pellets were optimized by single factor experiment and central composite design.The optimized formulation and technology were as follows: speed was 400r/min,the quantity of feeding was 80 g,the proportion of glycerol monostearate and stearic acid was 8:3,the amount of binder was 60.35%,the amount of sodium bicarbonate was 6.875%,and the amount of HPMC K100 was 13.83%.The shape of the floating micro pellets was regular,the particle size was uniform,and the floating time was more than 8h.The curcumin gastric floating micro pellets exhibited good sustained-release characteristics,and the drug release was in accordance with diffusion/ dissolution model.Curcumin niosomes were prepared by film dispersion method.With encapsulation efficiency as index,the formulation and technology of curcumin niosomes were optimized by single factor experiment and central composite design.The optimized formulation and technology were as follows: the ratio of Span80 to cholesterol was 4.2:1,the ratio of cholesterol to curcumin was 5:1,PBS volume was 20.9m L,hydration speed was 381r/min,hydration time was 1.5h,ultrasonic time was 3min,hydration temperature was 50?.The encapsulation efficiency of curcumin niosomes was 88.5%,average particle size was 162 nm,the Zeta potential was(-28.9±2.7)mV,and the shape was regular.The curcumin niosomes exhibited sustained-release characteristics,and the drug release was in accordance with Ritger-peppas model.The bioavailability of curcumin gastric floating micro pellets and niosomes was studied in rabbits.The time to peak of curcumin gastric floating micro pellets was significantly longer than that of curcumin common tablets(2.514±0.056 h,1.378±0.023h);the mean residence time(MRT(0-t))was significantly prolonged(6.120±0.266 h,2.512±0.018h);the area under the concentration time curve(AUC(0-t))was significantly increased(1631.178±128.860 ng·mL-1·h,601.409±3 3.036 ng·mL-1·h);and the relative bioavailability of curcumin gastric floating micro pellets was 271.23%,which was obviously improved.The time to peak of curcumin niosomes was longer than that of curcumin suspensions(1.868±0.378 h,1.226±0.012h);the mean residence time(MRT(0-t))was significantly prolonged(6.604±0.209 h,2.498±0.016h);the area under the concentration time curve(AUC(0-t))was significantly increased(2074.989±1 46.690ng·mL-1·h,803.475±23.335 ng·m L-1·h);and the relative bioavailability of curcumin niosomes was 258.25%,indicating that the bioavailability was significantly improved.