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Updated: Aug 5, 2026

Through the Looking Glass: Time-lapse Microscopy and Longitudinal Tracking of Single Cells to Study Anti-cancer Therapeutics
06:00

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Published on: May 14, 2016

Vorinostat nanoformulation triggers cell cycle blockade and apoptosis for colorectal cancer therapy

Leilei Yang1, Tingting Guo2, Junjun Chen3

  • 1School of Pharmaceutical Sciences, Jilin University, Changchun 130021, China.

International Journal of Pharmaceutics
|August 3, 2026
PubMed

Insights

A novel targeted nanoformulation effectively delivered vorinostat (VOR) to colorectal cancer (CRC) cells, enhancing apoptosis and suppressing tumor growth. This targeted delivery overcomes limitations of traditional vorinostat therapy for CRC.

Area of Science:

  • Oncology
  • Nanomedicine
  • Pharmacology

Background:

  • Colorectal cancer (CRC) is a leading cause of cancer mortality globally.
  • Histone deacetylase (HDAC) inhibitors like vorinostat (VOR) show anti-cancer potential but face delivery challenges.
  • Limitations include rapid clearance, poor tumor distribution, and off-target effects of VOR.

Purpose of the Study:

  • To develop and evaluate a targeted nanoformulation for enhanced VOR delivery in CRC.
  • To overcome the pharmacokinetic and biodistribution limitations of free VOR.

Main Methods:

  • Fabrication of a targeted nanoformulation (T-NP.VOR) using PLGA-PEG-AEAA.
  • In vitro assessment of cellular uptake, HDAC inhibition, cell cycle arrest, and apoptosis in CRC cells.
  • In vivo evaluation in an orthotopic CRC mouse model, assessing pharmacokinetics, tumor distribution, tumor growth, and survival.

Main Results:

  • T-NP.VOR demonstrated enhanced cellular uptake in CRC cells via Sigma-1 receptor-mediated endocytosis.
  • In vitro studies showed T-NP.VOR induced HDAC inhibition, cell cycle arrest, and apoptosis.
  • In vivo, T-NP.VOR exhibited prolonged circulation, improved tumor accumulation, significant tumor suppression, and extended survival.

Conclusions:

  • The PLGA-PEG-AEAA nanocarrier is a promising platform for targeted VOR delivery in CRC.
  • This nanoformulation effectively addresses VOR's limitations, offering a potential therapeutic strategy for colorectal cancer.
Keywords:
Drug deliveryNanoparticleTargeted therapyVorinostat

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