Human serum albumin (HSA) nanoparticles have been widely used as versatile drug delivery systems for improving the efficiency and pharmaceutical properties of drugs. The present study aimed to design HSA nanoparticle encapsulated with the hydrophobic anticancer pyridine derivative (2-((2-([1,1'-biphenyl]-4-yl)imidazo[1,2-a]pyrimidin-3-yl)methylene)hydrazine-1-carbothioamide (BIPHC)). The synthesis of HSA-BIPHC nanoparticles was achieved using a desolvation process. Atomic force microscopy (AFM) analysis showed the average size of HSA-BIPHC nanoparticles was 80.21 nm. The percentages of entrapment efficacy, loading capacity and production yield were 98.11%, 9.77% and 91.29%, respectively. An In vitro release study revealed that HSA-BIPHC nanoparticles displayed fast dissolution at pH 7.4 compared to pH 3.4. They have also showed a higher cytotoxic activity against MCF-7 human breast cancer cells. The possible binding of the BIPHC into the tyrosine threonine kinase (TTK) was studied using molecular modeling. The findings of this study introduced a promising candidate model of HSA nanoparticles for delivering of BIPHC anticancer drug. These novel nanoparticles are characterized by their ability to carry a hydrophobic BIPHC agent and control drug release with improved targeting of breast cancer cells.
