Preparation And Evaluation Of Curcumin-Loaded Nanostructured Lipid Carriers

Curcumin is extracted from the root and stem of turmeric,the chemical structure of which contains aβ-diketone polyphenol.Curcumin exhibits anti-oxidation,anti-inflammatory,anti-bacterial,anti-virus and anti-tumor activities.In recent years,many researches demonstrated that curcumin exhibited anti-AD activity.However,curcumin has lower water solubility,rapid half-life period and lower bioavailability bringing to difficulty in clinic.Hence,the design of appropriate drug delivery system is urgently needed to improve the stability and bioavailability.Nanostructured lipid carrier(NLC)is lipid nanoparticles which is composed of solid lipid and liquid lipid.It displays high encapsulation rate.In this research,we constructed curcumin nanostructured lipid carriers(CUR-NLC)to improve the load capacity and the bioavailability of curcumin.Triphenylphosphine modifier to polyethylene glycol mono stearate(TPP-PS)was applied in the curcumin nanostructured lipid carrier modification.First,melting emulsification and ultrasonic dispersion methods were used to prepare NLC.The best formula and preparation technology according to diameter.The diameter,morphology,encapsulation efficiency and drug release preparation were detected.Then the reactive oxygen species scavenging activities in vitro and primary pharmacokinetic study in vivo were studied.The results show that CUR-NLC displays sphere microscopic morphology with particle size of 120 nanometer,electrically positive,encapsulation efficiency of 90.75±0.24%and slow-release characteristics.The CUR-NLC is stable in 4 ~oC condition.The results of antioxidant test demonstrated that it exhibits superior anti-oxidation ability in vitro.Pharmacokinetic study showed that CUR-NLC exhibit high peak concentration and larger AUC compared with that of CUR.Mice brain distribution assays shown that higher drug peak concentration and AUC were observed in CUR-NLC group compared with that of CUR group.This result was consistent with result of blood concentration test assays,indicating that NLC could improve the concentration and bioavailability of CUR.The CUR-NLC improved the water solubility,and bioavailability of curcumin.The research provided a scientific foundation for novel formulation design of curcumin.