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New Abstraction Technics Of Flavones And Terpene From Propolis And Nano-praeparatum

Posted on:2006-09-12Degree:DoctorType:Dissertation
Country:ChinaCandidate:Z G ChengFull Text:PDF
GTID:1101360182968625Subject:Surgery
Abstract/Summary:PDF Full Text Request
Propolis is a honeybee product with a broad spectrum of biological activities and therapeutic properties, including antimicrobial, anticarcinogenic, immunomodulatory, antioxidant, anti-inflammatory activities, among others. The main pharmacologically active molecules in the propolis are flavonoids. Because of its physiological activities and pharmacological properties, bioflavonoids have attracted attention from the field of medication and delicatessen. It's necessary that carrier for bioflavonoids to improve their bioavailability and targeting.Nanoparticles drug carrier system offer a number of advantages as colloidal drug delivery, and become a research hotspot in biomedicine. Solid lipid nanoparticles are solid delivery carrier of drugs in a lipid matrix, using lecithin, Stearic acid and others as carrier. Particle diameters are among 50 and 1000 nm. Solid lipid nanoparticles offer a number of potential advantages as delivery systems, such as better bioavailability for poorly water-soluble drugs, higher drug loading capacity, lower toxicity, targeted drug delivery, allowing large scale production and others. Surface modified solid lipid nanoparticles by polyethylene glycol furnish other advantages such as lower targeting to reticulation endothelium system, lower distribution in reticulation endothelium system and extending circulation time in vivo.Based on the above progresses, Stearic acid solid lipid nanoparticles were utilized as a drug carrier system containing propolis flavones, the surface of nanoparticles modified by polyethylene glycol. Modified by polyethylene glycol Stearic acid solid lipid nanoparticles containingpropolis flavones were prepared in order to improving bioavailability of oral using propolis flavones, reducing targeting to mononuclear phagocyte system (MPS) and transforming tissue distribution of propolis flavones. The potential of SLN to be exploited as oral administration of nanoparticles drug carrier of propolis flavones for treatment of cardiovascular and cerebrovascular disease and diabetes mellitus is highlighted.In this study, we have separated the flavones from propolis by ethanol endosmosis and ester extraction and the purity of flavones in propolis extracts was 36.7% determined by ultraviolet spectrophotometer. The purification of propolis extracts was isolated with a silica gel column and gained propolis flavones and the purification of them was 70.94% determined by ultraviolet spectrophotometer. Here furnishes the material for preparation of Stearic acid solid lipid nanoparticles containing propolis flavones.To prepare Modified by polyethylene glycol Stearic acid solid lipid nanoparticles containing propolis flavones according with design qualification, the method of 'emulsion evaporation-solidification at low temperature' was used to prepare the nanoparticles, and optimize the preparation technics by Orthogonal Design. The diameter of modified by polyethylene glycol Stearic acid solid lipid nanoparticles containing propolis flavones prepared by optimized the preparation techniques is (238.6±30.1) nm, its drug loading is 14.2% and its entrapment efficiency is 74.9%. The surface modified nanoparticles by Brij78 may reduce the uptake by mouse peritoneal macrophage. The in vitro release characteristics investigated fitted to first-order pharmacokinetic model,and the in vitro release mathematics model is Q=1.5876+3.6777t— 0.03 9 It2.Based on the above the in vitro release characteristics, we study the pharmacokinetics of PEG-PF-PA-SLN by oral administration in rabbits. The results show that the bioavailability was improved, tissue distribution was modified and the content of propolis flavones was increased significantly by oral administration of PEG-PF-SA-SLN in rabbit.Based on the above the researches, we study the pharmacological properties in SD rats with diabetes mellitus. The results show that the level of blood glucose was decreased significantly between Group propolis flavones and Group PEG-PF-SA-SLN in the SD rats with diabetes mellitus. The level of blood glucose in Group PEG-PF-SA-SLN is lower significant than that in Group propolis flavones. The mechanism of treatment of diabetes mellitus by propolis flavones may be suppressing lipid peroxidation, reducing nitric oxide, repairing P-cells in pancreas and facilitating exudation insulin. Suppressing lipid peroxidation and protecting the activity of Na+-K+-ATPase of RBC membranes may be beneficial to prevention and cure of diabetes mellitus and correlative complication.In summary, we have separated and purified the flavones from propolis and gained propolis flavones and the purification of them was 70.94%. The method of 'emulsion evaporation-solidification at low temperature' was used to prepare PEG-PF-PA-SLN. The pharmacological research shows the rate of drug release of PEG-PF-PA-SLN is slow in vivo and in vitro. The content of propolis flavones was increased significantly by oral administration of PEG-PF-SA-SLN in rabbit. Thelevel of blood glucose in Group PEG-PF-SA-SLN is lower significant than that in Group propolis flavones. The mechanism of treatment of diabetes mellitus by propolis flavones may be suppressing lipid peroxidation, reducing nitric oxide, repairing [3-cells in pancreas and facilitating exudation insulin.
Keywords/Search Tags:propolis, flavones, carrier, lipid, nanoparticles, pharmacology, diabetes mellitus
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