4.7 Review

Recent advances in nanomedicine-based delivery of histone deacetylase inhibitors for cancer therapy

Journal

NANOMEDICINE
Volume 16, Issue 25, Pages 2305-2325

Publisher

FUTURE MEDICINE LTD
DOI: 10.2217/nnm-2021-0196

Keywords

cancer drug resistance; drug delivery; epigenetics; HDAC inhibitors; nanoparticles

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Histone deacetylase inhibitors (HDACi) are cancer therapeutics that operate at the epigenetic level. Nanocarriers can overcome limitations of HDACi, offering enhanced tumor targeting, improved cellular uptake, and reduced toxicity. Engineered stimuli-responsive nanosystems allow for site-specific drug delivery.
Histone deacetylase inhibitors (HDACi) are cancer therapeutics that operate at the epigenetic level and which have recently gained wide attention. However, the applications of HDACi are generally hindered by their poor physicochemical characteristics and 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 and reduced 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 review we elucidate the anticancer mechanisms of HDACi and their structure-activity relationships, with a special focus on their nanomedicine-based delivery, different drug loading concepts and their implications.

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