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Research On Drug Delivery System Of Cationtic Syringopicroside Peg-plga Nanoparticles Modified By HBsAg

Posted on:2015-03-07Degree:MasterType:Thesis
Country:ChinaCandidate:X L ChenFull Text:PDF
GTID:2254330428475470Subject:Pharmacy
Abstract/Summary:PDF Full Text Request
The purpose of the present work was to develop hepatitisB surface antigen (HBSAg) surface-adsorbed cationic PEG-PLGA nanoparticles for Syringopicroside(SYR) delivery targeted to hepatocytes.This study aim was to explore Polyethylene-glycol-Polylactic-co-glycolic acid (PEG-PLGA) as the carrier of the nanoparticles SYR material preparation, morphological characteristics and the body of drug release characteristics. This lab mainly on the following aspects:1Preparition cationic PEG-PLGA blank nanoparticles.This experiment elects three kinds of methods to prepare the cationic PEG-PLGA blank nanoparticles and the preparation process uses three different aqueous phase, and characterize for the prepared nanoparticles.And finally elects the best method of double emulsion solvent evaporation method, and the web of the phase to the aqueous solution of CTAB and tween80, The surface potential for prepared particles is+45mV, and the average particle size is within70nm.2Cationic Syringopicroside PEG-PLGA nanoparticles modified by HBSAg nucleoside preparation.The complex method,the emulsification SYR-PEG-PLGA nanopart-icles modified by HBSAgto the encapsulation efficiency as the main index, by orthogonal experiment design, determined the best prescription:SYR dosage of15mg/mL, PEG-PLGA dosage of10mg/mL, The proportion of water phase and a the organic phase for1:5proportion. Seal the bag rate is60.1plus or minus1.21%, the drug for6.01plus or minus0.21%. The transmission electron microscope in the form is kind of round sphere entity particle, particle size distribution is uniform, and the average particle size for (131.4±0.93) nm.3Cationic Syringopicroside PEG-PLGA nanoparticles modified by HBSAg reeze-dried preparation.A freeze-drying method was investigated in order to improve the stability of the SYR-PEG-PLGA-NP modified by HBSAg,and the best prescription was selected by screening protector and its concentration. The results showed that using5%mannitol as a protector was better.4Cationic Syringopicroside PEG-PLGA nanoparticles modified by HBSAg in vitro release. By using dynamic dialysis method to study SYR-PEG-PLGA nanoparticles modified by HBSAgin37℃, pH7.4phosphate buffer of drug release of properties. Test results show that36hours in vitro release88.07%, SYR-NP freeze-dried in vitro release with the basic law Higuchi equation of drug release model. Fitting of drug release kinetics equation for:Q=0.1281+0.0189t1/2(r=0.9568) in vitro test results show that the SYR-PEG-PLGA nanoparticles modified by HBSAghave good slow-release features.5Cationic Syringopicroside PEG-PLGA nanoparticles modified by HBSAg targeting of liver in mice.Mouse tail vein injection of SYR-PEG-PLGA-NP modified by HBSAg solution and cloves gentiopicroside solution,HPLC method to detect the concentration of tissue cloves gentiopicroside,Gentiopicroside trapezoidal method clove in each organization accumulation in mice.In drug selectivity index (re) and drug targeting index (te).Evaluation distribution in mice after administration of cationic Syringopicroside PEG-PLGA nanoparticles modified by HBSAgnanoparticles. The results show that teare greater than1of Syringopicroside and cationic Syringopicroside PEG-PLGA nanoparticles modified by HBSAg nanoparticles,and the latter is twice.This shows that the Syringopi-croside monomer itself in the liver is more selective distribution, consistent with the Syringopicroside hepatoprotective effect,On the other hand also shows what is made of SYR-PEG-PLGA-NPmodified by HBSAg,. improves the liver tissue distribution of Syringopicroside, better plays the role of liver targeting. At the same time, re is1.97, also shows that S YR-PEG-PLGA-NPmodified by HBSAg has a good liver targeting.By researching on cationic PEG-PLGA nanoparticles loaded with SYR,it were prepared by the double emulsion solvent evaporation method in the end.Delipidated HBSAg was passively adsorbed on the surfaceof nanoparticles by using the simple dipping and dryingmethod. Surface morphology and size distribution ofnanoparticles were analyzed by scanning electronmicroscopy and dynamic light-scattering method, respectively.The biodistribution behavior of cationicSyringopicroside PEG-PLGA nanoparticles modified by HBSAg nanoparticles was alsoexamined followed by intravenous injection.The results show that SYR-PEG-PLGA-NP modified by HBSAg in liver of re was1.97, and the SYR-PEG-PLGA-NPof rewas1.63,re>1, proves that cationic SYR-PEG-PLGA-NP modified by HBSAg and the SYR-PEG-PLGA-NP targeted to the liver better, can obviously improve the distribution of Syringopicroside in the liver,From the targeting efficiency (te)for the liver targeting property,nanoparticles group was obviously greater than Syringopicroside solution group, and itshows that the modified nanoparticles can soon concentration in the liver after intravenous injection concentration, so as to achieve the goal of liver targeting. Accordingly, it also proves that SYR-PEG-PLGA nanoparticles modified by HBSAg significantly increased the drugs liver targeting property after surface modification.
Keywords/Search Tags:Syringopicroside, PEG-PLGA, Nanoparticles, Double emulsion solvent evaporation method, In vitro drug release, Pharmacokinetics
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