PEGylated polycyanoacrylate nanoparticles as tumor necrosis factor-α carriers

• Published in: Journal of controlled release 2001-04, Vol.71 (3), p.287-296
• Main Authors: Li, Ya-Ping, Pei, Yuan-Ying, Zhou, Zhao-Hui, Zhang, Xian-Ying, Gu, Zhou-Hui, Ding, Jian, Zhou, Jian-Jun, Gao, Xiu-Jian
• Format: Article
• Language: English
• Subjects: Biological and medical sciences; Chemical Phenomena; Chemistry, Physical; Cyanoacrylates - chemistry; Drug Carriers; Drug Stability; General pharmacology; human serum albumin; Humans; Medical sciences; methoxy-polyethyleneglycol cyanoacrylate; Microspheres; n-hexadecyl cyanoacrylate; Nanoparticles; Pharmaceutical technology. Pharmaceutical industry; Pharmacology. Drug treatments; Poly(alkyl cyanoacrylate); Poly(ethylene glycol); Poly(methoxy-polyethyleneglycol cyanoacrylate-co- n-hexadecy cyanoacrylate); polycyanoacrylate; Polyethylene Glycols - chemistry; Recombinant human tumor necrosis factor-α; Recombinant Proteins - chemistry; Solubility; Solutions; Tumor Cells, Cultured; Tumor Necrosis Factor-alpha - administration & dosage; Tumor necrosis factor-α
• ISSN: 0168-3659; 1873-4995
• DOI: 10.1016/S0168-3659(01)00235-8

The aim of this study was to find an effective carrier for recombinant human tumor necrosis factor-α (rHuTNF-α). The influence of solvent systems containing poly(methoxy-polyethyleneglycol cyanoacrylate-co- n-hexadecyl cyanoacrylate) (PEGylated PHDCA) on the biological activity of rHuTNF-α was investigated. The PEGylated PHDCA nanoparticles loading rHuTNF-α were prepared with the double emulsion method. The influence of main experimental factors on the entrapment efficiency was evaluated by the Uniform Design. The physicochemical characteristics and in vitro release of rHuTNF-α from the nanoparticles were determined. The results showed that serum albumin such as human serum albumin (HSA) or bovine serum albumin (BSA) could play a protective action on rHuTNF-α in the preparation process. At ≥2.0% (w/v) HSA concentration, more than 85% of rHuTNF-α activity remained and the role of HSA was not affected by copolymer concentrations from 0.5 to 3.0% (w/v). The entrapment efficiency of the nanoparticles was about 60% and the nanoparticle size was about 150 nm. The nanoparticles were spherical in shape and uniform with the value of the zeta potential about −9 mV. The rHuTNF-α release from the nanoparticle showed an initial burst and then continued in a sustained fashion. The results showed that the PEGylated PHDCA nanoparticles could be an effective carrier for rHuTNF-α.