مختصر البحث:
Introduction
Bortezomib (BTZ) is a proteasome inhibitor approved for the treatment of multiple myeloma. It is under investigation for use in the treatment of other solid tumors, such as breast and prostate cancers. BTZ is known for its high potency…
Introduction
Bortezomib (BTZ) is a proteasome inhibitor approved for the treatment of multiple myeloma. It is under investigation for use in the treatment of other solid tumors, such as breast and prostate cancers. BTZ is known for its high potency, limited aqueous solubility, and systemic toxicity. These characteristics restrict its clinical application. This study aims to formulate BTZ in the form of bovine serum albumin (BSA) nanoparticles (NPs) to enhance its anticancer targeting. The Box–Behnken experimental design was employed to optimize the formulation of BTZ-loaded BSA NPs.
Methods
BTZ BSA NPs were prepared through the desolvation method by using glutaraldehyde (Glut) as a crosslinker. The Box–Behnken design was employed as an experimental design tool to investigate the impact of formulation parameters, specifically the amount of BTZ, BSA, and antisolvent volume, on outcomes, including particle size (PS), entrapment efficiency (EE%), and polydispersity index (PDI). The morphology of the prepared NPs was examined using a transmission electron microscope (TEM), while a compatibility study was conducted using Fourier transform infrared spectroscopy (FTIR) and differential scanning calorimetry (DSC).
Results
The optimized formulation resulted in a mean PS, EE%, and PDI of 74 nm, 68%, and 0.007, respectively. The BTZ BSA NPs exhibited a sustained in vitro release profile over 24 hours. TEM revealed that the prepared NPs had an almost spherical morphology. FTIR and DSC revealed that BTZ was encapsulated well within the prepared NPs with minimal decomposition and/or degradation.
Discussion
The optimized BTZ BSA NPs exhibited uniform nanosize, high entrapment efficiency, and sustained drug release, confirming the effectiveness of Box–Behnken optimization. Encapsulation within the cross-linked albumin matrix protected BTZ from hydrolytic degradation, enhanced its stability, and provided controlled release, supporting its potential for improved anticancer activity and reduced systemic toxicity.
Conclusion
The use of experimental design is a valuable tool for optimizing the formulation of BTZ BSA NPs, achieving the required PS, high EE%, and low PDI
