Bortezomib (VELCADE®) is a boronate peptide and first-in-class proteasome inhibitor serving an
important role in degenerating several intracellular proteins. It is a reversible inhibitor of the 26S proteasome,
with antitumor activity and antiproliferative properties. This agent principally exerts its antineoplastic effects by
inhibiting key players in the nuclear factor κB (NFκB) pathway involved in cell proliferation, apoptosis, and
angiogenesis. This medication is used in the management of multiple myeloma. However, more recently, it has
been used as a therapeutic option for mantle cell lymphoma. While promising, bortezomib has limited clinical
applications due to its adverse effects (e.g., hematotoxicity and peripheral neuropathy) and low effectiveness in
solid tumors resulting from its poor penetration into such masses and suboptimal pharmacokinetic parameters.
Other limitations to bortezomib include its low chemical stability and bioavailability, which can be overcome by
using nanoparticles for its delivery. Nanoparticle delivery systems can facilitate the targeted delivery of chemotherapeutic
agents in high doses to the target site, while sparing healthy tissues. Therefore, this drug delivery
system has provided a solution to circumvent the limitations faced with the delivery of traditional cancer chemotherapeutic
agents. Our aim in this review was to describe polymer-based nanocarriers that can be used for the
delivery of bortezomib in cancer chemotherapy.