Study Of Ginkgolides Pelge Nano Rice

Ginkgolides are a group of unique terpene lactones extracted from ginkgobiloba. They have important bioactivities with specific structure andpharmacological properties. GG are a series of specific platelet activatingfactor(PAF) antagonists, they can inhibit the adhesion and aggregation of theplatelet, prevent thrombosis, and possess anticerebral ischemia effects. There aremany clinical applications just like treatment of coronary heart disease, cerebralthrombosis, cerebral thrombosis, cerebrovascular insufficiency, nervous systemdisease, suffocative catarrh. The bilobalides lacks PAF antagonistic activity butshows neuroprotective effects. Comparatively, GG have less toxic componentsand dosage than traditional ginkgo biloba extraction (GBE). The half life time ofGG is 2～3h, and long-term administration is needed.The main aims of this research were to develop GG PELGE nanoparticles(GG-PELGE-NP) with high bioavailability and long circulation in vivo. Themouse peritoneal macrophages were used to investigate the uptake characteristicsof nanoparticles in vitro. The GG-PELGE-NP was further developed topowders and the characteristics of the powders was also investigate. The in vitroreleasing characteristics of GG-PELGE-NP was studied. Finally, the studies onpharmacokinetics of GG-PELGE-NP were also determined.The mouse peritoneal macrophages were used to investigate the uptakecharacteristics of nanoparticles in vitro. The cell uptake characteristics ofRhodamine123-PLGA-NP and Rhodamine123-PELGE-NP were investigatedrespectively. We had investigated the molecular weight of PEG and the percent of PEG impact on the cell uptake characteristics and the effect of F₆₈.Comparatively, the results showed that the cell uptake percentage of PELGE-NPwas much lower than that of PLGA-NP. The molecular weight of PEG and thepercent of PEG had significant effect on MPM uptake percentage. PELGE plus 3% F₆₈ had better results.The GG-PELGE-NP was prepared by the procedure of "nanoprecipitation".The optimized formulation of GG-PELGE-NP was conveniently obtained by theL16(4⁴) orthogonal methodology. The uniform of GG-PELGE-NP was observedby transmission electron microscopy, while its particle size and Zeta potentialwere measured by Nicomp 380^TM Zeta Potential/Particle Sizer. The resultsshowed that the volume-weight mean particle diameter was 123～131nm, whilethe Zeta potential was-28～-33mV. The entrapment efficiency of GG was66.95±1.72%. The TEM photo proved that the GG-PELGE-NP was sphericalshape.The powders of the GG-PELGE-NP were prepared by lyophilization using2.5% lactose and 2.5% fucose as protector. We carried on the overall qualityevaluation to the lyophilization injection, the results showed that thelyophilization didn't influence the quality index of the GG-PELGE-NP, such assize, drug loading, pH etc. The crystallization behavior of the powders wasinvestigated by DSC. The results showed that they had formed a new materialphase. The results showed that the GG-PELGE-NP had good stability at the roomtemperature and 4℃.The in vitro releasing characteristics of GG-PELGE-NP was studied.Comparatively, the results showed that GG-PELGE-NP had remained releasingcharacteristics. The pharmacokinetic parameters of GG solution(GG-Sol) andGG-PELGE-NP were investigated after intravenous administration to rats at asingle dose of 8.79mg/kg. Comparatively, GG-PELGE-NP could prolong thecirculation of GG-Sol in blood and improve its bioavailability.