Dissertation > Medicine, health > Pharmacy > Drug basic science > Medicinal Chemistry

Study of Amphotericin B Magnetic Liposomes

Author ZhaoMengYu
Tutor GaoZiBin
School Hebei University of Science and Technology
Course Medicinal Chemistry
Keywords Amphotericin B Magnetic liposome Pharmacokinetics Tissues distribution Carotid artery injection Targeting
CLC R914
Type Master's thesis
Year 2014
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This study aims to prepare amphotericin B magnetic liposomes (AmB-MLPs), whichmay improve drug concentration and enhance magnetic targeting, resulting in reducingdrug toxicity in presence of magnetic field, subsequently we investigated its characters invivo and in vitro. AmB-MLPs were prepared by means of film dispersion-ultrasonication.The particle size and encapsulation efficiency were achieved under these optimizedprescription and preparation conditions determined by single factor experiment, and itsphysical properties were characterized. Three administration types were designed,including AmB injection, AmB-MLPs in absence of magnetic field and AmB-MLPs inpresence of magnetic field in lung of KM mice by tail intravenous injection respectively.Pharmacokinetics, tissues distribution and lung targeting of AmB-MLPs were studied.Furthermore, three administration types were injected by carotid artery in SD rats, and itsbrain targeting in magnetic field was investigated. The mean size of particles was250±12nm, the mean encapsulation efficiency was78.02±2.05%, and the saturation magnetizationwas32.54memu·g-1at room temperature, which has good magnetic responsiveness.Pharmacokinetics results of KM mice showed that t1/2β, MRT and AUCt wereobviously increased, while CL was decreased in the group of AmB-MLPs in presenceof magnetic field than that of AmB injection. These results indicated that AmB-MLPs inpresence of magnetic field could prolong the time in the blood circulation. AmB-MLPsnot only improved passive targeting in liver and spleen, but also enhanced magnetictargeting in lung in presence of magnetic field. Furthermore, the drug concentration inbrain was increased to a certain extent via the carotid artery injection. The concentrationof drug in the brain was further enhanced when the magnetic field was applied in the brain.The Prussian blue staining in brain of SD rats showed that the density of bluestaining-positive particles in brain tissue of applying magnetic field group was higher thanthat of non magnetic field group. These results suggested that AmB-MLPs could reinforcebrain targeting when they were injected by carotid artery under the effect of magnetic field.In a word, AmB-MLPs could enhance magnetic targeting and then reduce drug toxicreaction in presence of magnetic field.

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