Effect of MePEG molecular weight and particle size on in vitro release of tumor necrosis factor-α-lo

来源 :Acta Pharmacologica Sinica | 被引量 : 0次 | 上传用户:comboyaoqiu
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Aim:To study the in vitro release of recombinant human tumor necrosis factor-alpha(rHuTNF-α)encapsulated in poly(methoxypolyethyleneglycol cyanoacry-late-co-n-hexadecyl cyanoacrylate)(PEG-PHDCA)nanoparticles,and investigatethe influence of methoxypolyethyleneglycol(MePEG)molecular weight and par-ticle size.Methods:Three sizes(approximately 80,170,and 240 nm)of PEG-PHDCA nanoparticles loading rHuTNF-α were prepared at different MePEG mo-lecular weights(M_r=2000,5000,and 10000)using the double emulsion method.The in vitro rHuTNF-α release was studied in PBS and rat plasma.Results:Ahigher burst-release and cumulative-release rate were observed for nanoparticleswith higher MePEG molecular weight or smaller particle size.A decreased cu-mulative release of rHuTNF-α following the initial burst effect was found in PBS,while the particle sizes remained constant and MePEG liberated.In contrast,inrat plasma,slowly increased cumulative-release profiles were obtained after theburst effect.During a 5-h incubation in rat plasma,more than 50% of the PEG-PHDCA nanoparticles degraded.Conclusion:The MePEG molecular weightand particle size had an obvious influence on rHuTNF-α release,rHuTNF-αreleased from PEG-PHDCA nanoparticles in a diffusion-based pattern in PBS,but in a diffusion and erosion-controlled manner in rat plasma. Aim: To study the in vitro release of recombinant human tumor necrosis factor-alpha (rHuTNF-alpha) encapsulated in poly (methoxypolyethyleneglycol cyanoacrylate) (PEG-PHDCA) nanoparticles, and investigate the influence of methoxypolyethyleneglycol (Approximately 80,170, and 240 nm) of PEG-PHDCA nanoparticles loading rHuTNF-α were prepared at different MePEG mo-lecular weights (M_r = 2000, 5000, and 10000) using the double emulsion method. in vitro rHuTNF-α release was studied in PBS and rat plasma. Results: Ahigher burst-release and cumulative-release rate were observed for nanoparticles with higher MePEG molecular weight or smaller particle size. A decreased cu-mulative release of rHuTNF-α following the initial burst effect was found in PBS, while the particle sizes remained constant and MePEG liberated. In contrast, inrat plasma, slowly increased cumulative-release profiles were obtained after the burst effect. Durin ga 5-h incubation in rat plasma, more than 50% of the PEG-PHDCA nanoparticles degraded. Conlusion: The MePEG molecular weight and particle size had an obvious influence on rHuTNF-α release, rHuTNF-αreleased from PEG-PHDCA nanoparticles in a diffusion -based pattern in PBS, but in a diffusion and erosion-controlled manner in rat plasma.
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