Preparation And Characterization Of Curcumin Chitosan-Oleyl Micells

Objective:In this work, we firstly synthesised the oleyl-chitosan materials, created appropriate aqueous environment, and the materials formated the micelles self-assembly. We used the CUR as the model drug, prepared the drug-loaded micelles. In a word, the durg-loaded micells had the ability of high effectivity, long term, low side effect. So it provided a new technological method for anti-cancer drugs.Methods:(1) Preparation and characterization of CUR-Oleyl-CS micellesCUR-Oleyl-CS micelles had been prepared by dialysis method. The size, zeta potential and drug loading were evaluated to optimize the parameters of materials content, drug concent, power and time of ultrasound.The size, zeta potential were characterized by Zetasizer Nano system. The drug loading was measured by the method of UV and HPLC at420nm. The study of drug release of drug-loaded micelles was performed by dialysis method. According to the changes of Zeta potential, the storage stability was decided at4℃and25℃. (2) Study of the antitumor activity of CUR-Oleyl-CS micelles in vitro The influences of growth inhibition of CUR-Oleyl-CS micelles and free CUR were carried on MCF-7cells by MTT assay. The apoptosis effect of CUR-Oleyl-CS micelles on cells was studied.Results:(1) The best prepared condition was as followed:materials=100mg, drug=10mg, time=10min, and power of ultrasound=60W. In this condition, the CUR-Oleyl-CS micelles were spherical in shape and narrow in distribution. The average size of micelles were (105±2.58) nm, the zeta potential was+(25.52±5.21) mV, and the encapsulation ratio was (26.7±4.17)%. The drug release of CUR-Oleyl-CS micelles in viro had the characteristic of controlling release. CUR released from CUR-Oleyl-CS micelles was faster in the first40min, then entered into release platform phase, and almost released completely after4days. The micelles were almost stabilized for at3months, and there were phase separation in3months. With the extension of time, the zeta potential reduced.(2) Both CUR-Oleyl-CS micelles and free CUR killed the MCF-7. And the IC50of CUR-Oleyl-CS micelles on MCF-7cells were6.25μg/mL、3.37μg/mL、1.68μg/mL,(compared to free CUR, P<0.05). The accumulation of FITC in MCF-7cells increased compared with that of free FITC. After treatment with CUR-Oleyl-CS micelles, there were obvious cell apotosis. And the cells were restrainted at G2by CUR-loaded micelles.Conlusions:The novel cationic CUR-Oleyl-CS micelles enhanced the anticancer activity. Meanwhile, the micelles had better physicochemical property. As a result, this kind of drug-loaded micelles can act as the most promising drug carrier of hydrophobic drugs.