Abstract

Human serum albumin (HSA) nanoparticles hold great promise as a nanocarrier system fortargeted drug delivery. The objective of this study was to explore the possibility ofpreparing size controllable albumin nanoparticles using the disulfide bond breaking reagentβ-mercaptoethanol(β-ME). The results showed that the protein concentration and temperaturehad positive effects on the sizes of the albumin nanoparticles, while pH hada negative effect on the rate of nanoparticle formation. The addition ofβ-ME induced changes in HSA secondary structure and exposed the hydrophobic core ofHSA, leading to the formation of nanoparticles. Human serum albumin nanoparticles couldbe internalized by MCF-7 cells and mainly accumulated in cytoplasm. After injectionin tumor bearing mice, the HSA nanoparticles accumulated in tumor tissues,demonstrating the targeting ability of the nanoparticles. Therefore, human serumalbumin can be fabricated into nanoparticles by breaking the disulfide bonds andthese nanoparticles exhibit high tumor targeting ability. Human serum albuminnanoparticles could be ideal for the targeted delivery of pharmacologically activesubstances.

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