Aim: To study the in vitro release of recombinant human tumor necrosis factor‐alpha (rHuTNF‐α) encapsulated in poly (methoxypolyethyleneglycol cyanoacrylate‐co‐n‐hexadecyl cyanoacrylate) (PEG‐PHDCA) nanoparticles, and investigate the influence of methoxypolyethyleneglycol (MePEG) molecular weight and particle size.
Methods: Three sizes (approximately 80, 170, and 240 nm) of PEGPHDCA nanoparticles loading rHuTNF‐α were prepared at different MePEG molecular weights (Mr=2000, 5000, and 10 000) using the double emulsion method. The in vitro rHuTNF‐α release was studied in PBS and rat plasma.
Results: A higher burst‐release and cumulative‐release rate were observed for nanoparticles with higher MePEG molecular weight or smaller particle size. A decreased cumulative release of rHuTNF‐α following the initial burst effect was found in PBS, while the particle sizes remained constant and MePEG liberated. In contrast, in rat plasma, slowly increased cumulative‐release profiles were obtained after the burst effect. During a 5‐h incubation in rat plasma, more than 50% of the PEGPHDCA nanoparticles degraded. Conclusion: The MePEG molecular weight and particle size had an obvious influence on rHuTNF‐α release. rHuTNF‐α released from PEG‐PHDCA nanoparticles in a diffusion‐based pattern in PBS, but in a diffusion and erosion‐controlled manner in rat plasma.