Study On Long - Circulating Nitroglycerin Nanostructured Lipid Carrier

Objective To preparing curcumin long-circulating nanostructured lipid carriers(mPEG2000-CUR-NLC)modified with mPEG2000-DSPE, and investigate their physicochemical properties.Methods Curcumin long-circulating nanostructured lipid carriers were prepared by thin-film dispersion and ultrasonication method, the particle diameter, the drug loading capacity andthe encapsulation efficiency were response variables, optimized procedure by using Box-Behnken experimental design based on the results of a single-factor test. The PD, EE DL andZeta DSC、XRD and The in vitro drug release rate. Using Aβ25-35-induced toxicity PC12cells toset up the cell model of Alzheimer’s disease（AD）.Then the cell hyperplasia was detected byMTT,effect of CUR on the expression of in PC12cells treated with Aβ25-35by RT-PCR.Results Under the optimal conditions, the designed nanoparticles showed nearly sphericalparticles with a mean particle diameter was (135.33±2.52)nm, Polydispersity Index(0.019±0.01),and drug loading was (2.41±0.587)%, entrapment efficiency was (96.70±0.146)%and Zeta potential was (-17.65±0.46)mV. mPEG2000-DSPE-CUR-NLC was freeze-dried with10%mannitol as lyoprotectant. Aβ25-35was induced PC12cells effective concentration at theconcentration of20.00μmol·L-1by MTT. The concentration at0.05~10.00μmol·L-1ofmPEG2000-DSPE-CUR-NLC could protect PC12cells against Aβ25-35toxicity damage. RT-PCRmeasurement result was shown that bcl-2mRNA expression was raised with mPEG2000-DSPE-CUR-NLC, inhibition of apoptosis.Conclusion Through thin-film dispersion and ultrasonic method produce mPEG2000-DSPE-CUR-NLC, uniform particle size distribution, better encapsulation efficiency andstability under optimization conditions by using Box-Behnken experimental design. The resultsof indicated protective action in vitro of CUR on Aβ25-35was higher than the CUR-NLCsolution and mPEG2000-DSPE-CUR.