To achieve sustained-release delivery of granulocyte-macrophage colony-stimulating factor(GM-CSF) with native state,reduced initial burst as well as steady blood concentration. METHODOLOGY:GM-CSF was loaded in solvent...
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To achieve sustained-release delivery of granulocyte-macrophage colony-stimulating factor(GM-CSF) with native state,reduced initial burst as well as steady blood concentration. METHODOLOGY:GM-CSF was loaded in solvent-resistant polysaccharide glassy particles via aqueous-aqueous *** protein-loaded polysaccharide particles were further encapsulated in PLGA matrix to get polysaccharide particle-PLGA composite microsphere. The novel glassy polysaccharide particle and composite microsphere were characterized for protein loading efficiency,particle size,protein integrity and in vitro release,Also the bioassay was assessed by proliferative ability of TF1 cells in the process of preparation and in vitro *** studies were carried out in rats administered subcutaneously. RESULTS and DISCUSSION:Scanning electron microscopy showed the GM-CSF-polysaccharide glassy particle were spherical and smooth in size range of 1-5 um. The drug loading efficiency ranged from 89%to 92%.The composite microspheres showed 20%less initial with a gradual sustained release for 30 ***-CSF extracted from the composite microspheres showed good stability without protein degradation products and structural integrity changes in the size-exclusion chromatography *** the result of bioactivity determined by TF1 cells suggests that the bioactivity was preserved in the process of preparation and in vitro *** study demonstrated that the plasma GM-CSF level was well controlled for 2 weeks by one injection of polysaccharide particle-PLGA composite microsphere. CONCLUSIONS:Using self-stand aqueous-aqueous emulsion is an effective and convenient way to pre-formulate delicate proteins into solvent-resistant polysaccharide particles for formulating polymer-based *** addition to protein stability,loading proteins into polysaccharide particles prior to microencapsulation may also improve protein release kinetics
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