Abstract
In this study, a folate-targeted pH-sensitive bortezomib conjugate was developed for cancer-specific drug delivery and therapy. The conjugate showed improved cellular uptake, penetration, and anticancer activity compared to free bortezomib, a bortezomib-mannitol derivative, and a PEGylated bortezomib conjugate in folate receptor overexpressing cancer cells and their 3D spheroids.