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ACTA Pharmaceutica Sciencia
2026 , Vol 64 , Num 2
Formulation of bortezomib human serum albumin nanoparticles, in vitro and in vivo evaluation
1 University of Kufa, College of Pharmacy, Department of Pharmaceutics, Najaf, Iraq2 University of Baghdad, College of Pharmacy, Department of Pharmaceutics, Baghdad, Iraq
DOI : 10.23893/1307-2080.APS64015 Viewed : 212 - Downloaded : 80 Bortezomib (BTZ) is a selective proteasome inhibitor whose anticancer activity results from disrupting regulated protein turnover, leading to apoptosis. It is highly potent but lacks specificity and shows limited activity against solid tumors. This project aims to formulate BTZ as Human Serum Albumin Nanoparticles (HSA NPs) to improve its sensitivity and selectivity towards solid tumors. These albumin nanoparticles enable both passive and active targeting. Passive targeting occurs through the enhanced permeation and retention (EPR) effect of nanoparticles, while the overexpression of albumin receptors on tumor cells facilitates active targeting. BTZ HSA NPs have been prepared using the desolvation method. In vitro characterisation involved particle size (PS), polydispersity index (PDI), entrapment efficiency (EE%), particle morphology, and an in vitro release study. The optimised formula was then evaluated for its anti-tumor activity in vivo using BALB/c mice, where the tumor volume was measured, and a histopathological analysis of the tumor tissue was performed. The optimised formula has PS, PDI, and EE% of (28) nm, 0.045, and 36%, respectively. The particles exhibit an almost spherical morphology and a controlled-release profile, with approximately 85% of BTZ released within 24 hours. On the other hand, in vivo, the NPs showed a significant decrease in tumor volume compared with the group that received only pure BTZ or phosphate-buffered saline (PBS). The histopathological study showed better tumor aggressiveness (lower mitotic count and nuclear pleomorphism), increased apoptosis, and improved immune cell infiltration. Formulation of BTZ as HSA NPs is a successful approach to enhance its activity and selectivity against cancer cells. The desolvation method is a reliable, reproducible method for obtaining these NPs. Keywords : Bortezomib, human serum albumin nanoparticles, anticancer targeting, proteosome inhibitors, tumor targeting