A nanoparticle-based formulation containing the poorly water-soluble, second-generation taxane analog docetaxel covalently conjugated to proprietary and as of yet undisclosed degradable linkers and encapsulated in polymers, with antineoplastic activity. Upon intravenous administration of nanoparticle-encapsulated docetaxel, the nanoparticles are able to accumulate at the tumor site due to the unique characteristics of the tumor's vasculature, while avoiding normal, healthy tissue. Docetaxel is released and becomes active upon cleavage from various linkers at a predetermined and controlled rate which is dependent on the properties of the proprietary linkers. In turn, active, unconjugated docetaxel binds to the beta-subunit of tubulin, stabilizes microtubules and inhibits microtubule disassembly. This prevents mitosis and results in tumor cell death. Compared to the administration of docetaxel alone, this formulation is able to increase docetaxel’s efficacy while avoiding systemic exposure, which minimizes its toxicity. By using different linkers, docetaxel can be released at various rates.