Analysis of HDACi-coupled Nanoparticles: Opportunities and challenges.

Kühne M*, Hofmann S*, Lindemann H, Cseresnyés Z, Dzierza A, Schröder D, Godmann M, Koschella A, Eggeling C, Fischer D, Figge MT, Heinze T, Heinzel T# (2023) Analysis of HDACi-coupled Nanoparticles: Opportunities and challenges. In: Humana, New York, NY (eds.) HDAC/HAT Function Assessment and Inhibitor Development. Methods in Molecular Biology 2589, pp. 129-144. Springer Protocols. ISBN: 978-1-0716-2787.

*equal contribution #corresponding author


Systemic administration of histone deacetylase inhibitors (HDACi), like valproic acid (VPA), is often associated with rapid drug metabolization and untargeted tissue distribution. This requires high-dose application that can lead to unintended side effects. Hence, drug carrier systems such as nanoparticles (NPs) are developed to circumvent these disadvantages by enhancing serum half-life as well as organ specificity.

This chapter gives a summary of the biological characterization of HDACi-coupled NPs in vitro, including investigation of cellular uptake, biocompatibility, as well as intracellular drug release and activity. Suitable methods, opportunities, and challenges will be discussed to provide general guidelines for the analysis of HDACi drug carrier systems with a special focus on recently developed cellulose-based VPA-coupled NPs.


Zoltán Cseresnyés
Marc Thilo Figge


doi: 10.1007/978-1-0716-2788-4_9

PMID: 36255622