Abstract
Histone deacetylase inhibitors (HDACi) are cancer therapeutics that operate at the epigenetic level and whichhave recently gained wide attention. However, the applications of HDACiare generally hindered by their poor physicochemical characteristicsand unfavorable pharmacokinetic profile. Inspired by the approved nanomedicine-based drugs in the market, nanocarriers could provide a resort to circumvent the limitations imposed by HDACi. Enhanced tumor targeting, improved cellular uptake andreduced toxicity are major advantages offered by HDACi-loaded nanoparticles. More importantly, site-specific drug delivery can be achieved via engineered stimuli-responsive nanosystems. In this reviewwe elucidate the anticancer mechanisms of HDACi andtheir structure-activity relationships, with a special focus on their nanomedicine-based delivery, different drug loading concepts and their implications.
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