Polymeric micelles of suberoylanilide hydroxamic acid to enhance the anticancer potential in vitro and in vivo.

AIM: To improve the bioavailability and anticancer potential of suberoylanilide hydroxamic acid (SAHA) by developing a drug-loaded polymeric nanomicellar system.

METHODS: SAHA-loaded Poly(ethylene glycol)-block-poly(caprolactone) (PEG-PCL) micelles were developed, and physico-chemically characterized. In vitro cellular uptake, viability and apoptosis-inducing ability of the SAHA-PEG-PCL micelles were investigated. In vivo anticancer activity was evaluated in C57BL/6 mice-bearing tumor.

RESULTS: The SAHA-PEG-PCL micelles had optimum size (∼130 nm) with an entrapment efficiency of approximately 67%. The SAHA-PEG-PCL induced stronger cell cycle arrest in G2/M phase leading to higher rate of apoptosis compared to free SAHA. SAHA-PEG-PCL demonstrated significant tumor suppression compared to free SAHA in vivo.

CONCLUSION: The physicochemical properties and the antitumor efficacy of SAHA were improved by encapsulating in polymeric micelles.