MicroRNA Biogenesis is Enhanced by Liposome-Encapsulated Pin1 Inhibitor in Hepatocellular Carcinoma

Theranostics
Dan SunYong Peng

Abstract

Hepatocellular carcinoma (HCC) is in an urgent need of new, effective therapies to reduce morbidity and mortality. We have previously demonstrated that peptidyl-prolyl cis/trans isomerase Pin1 is a potential target for HCC therapy, due to its pivotal role in HCC development through regulating miRNA biogenesis, and discovered the small molecule API-1 as a novel and specific Pin1 inhibitor. Despite its significant anti-HCC activity, the low water solubility and in vivo bioavailability of API-1 limit its clinical application. To address these issues, we herein developed a liposomal formulation of API-1 to improve API-1 delivery and enhance its anti-HCC efficacy. Methods: We designed and developed a nanoscale liposomal formulation of API-1, named as API-LP. Subsequently, the mean diameter, polydispersity, zeta potential, encapsulation efficiency and thermal properties of the optimization API-LP were characterized. The enhanced anti-HCC activity and the molecular mechanism of API-LP were investigated both in vitro and in vivo. Finally, the safety and pharmacokinetic property of API-LP were evaluated systematically. Results: API-LP had good formulation characteristics and exhibited an enhanced in vitro activity of suppressing prolife...Continue Reading

Citations

Feb 6, 2020·Frontiers in Cell and Developmental Biology·Chi-Wai Cheng, Eric Tse
Apr 17, 2020·Frontiers in Cell and Developmental Biology·Wenchen PuYong Peng

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Methods Mentioned

BETA
dynamic light scattering
flow cytometry
FACS
PCR
confocal microscopy
xenograft

Software Mentioned

GraphPad
GraphPad Prism

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