Antitumor effect and toxicity of an albumin-paclitaxel nanocarrier system constructed via controllable alkali-induced conformational changes

Various strategies have been developed to construct albumin nanomaterials via biophysical or chemical changes. In this work, a compound comprising albumin-paclitaxel nanoparticles (NPs-PTX) with a drug loading efficiency of 21% was constructed via manipulation of alkali induced conformation changes and hydrophilic-hydrophobicity transition. The toxicity of two PTX formulations (Taxol® and NPs-PTX) in human umbilical vein endothelial cells (HUVECs); RAW264.7, K562, and HepG2 cells; and rats were determined. The IC50 of Taxol® was remarkably lower than that of NPs-PTX. Both PTX formulations promoted cell apoptosis, possibly via mitochondria-dependent (intrinsic) and mitochondria-independent pathways. The effect of PTX formulations (0.5 to 1 mg mL-1) on hemolysis and the LD50 values of the PTX formulations were significantly different (p < 0.01). Reductions in the number of white blood cells (WBCs) and monocytes (MNCs) and obvious pathological changes in the spleen, thymus, and mesenteric lymph nodes were ob...