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Purpose <p>Colorectal cancer (CRC) is a leading digestive malignancy often diagnosed at advanced stages due to the absence of early biomarkers, resulting in poor prognosis. Effective drug delivery is crucial for improving outcomes. This study introduces FA-OHEC-APTES, a pH-responsive nano-drug delivery system, developed by modifying natural fibers (OHEC) with folic acid (FA) and 3-aminopropyltriethoxysilane (APTES) to enable targeted delivery, controlled release, and fluorescence tracking.</p> Methods <p>FA-OHEC-APTES was synthesized and characterized using FTIR, SEM, and nitrogen adsorption-desorption isotherms, confirming its porous nanoscale structure that facilitates drug loading and sustained release. Compound 1, a novel anti-CRC agent, was encapsulated to form FA-OHEC-APTES@1. Fluorescence spectroscopy evaluated pH-responsive drug release, while CCK-8 and qPCR assays assessed its therapeutic effects in HT29 colorectal cancer cells.</p> Results <p>FA-OHEC-APTES@1 exhibited pH-sensitive release, with 72.5% at pH 5.5 versus 35.8% at pH 7.4, aligning with the acidic tumor microenvironment. CCK-8 assays revealed dose-dependent inhibition of HT29 proliferation, with 70% viability reduction at 30 µM (<i>P</i> &lt; 0.01). qPCR analysis showed 45% downregulation of EZH2, suggesting epigenetic modulation.</p> Conclusion <p>FA-OHEC-APTES@1 demonstrates acidic tumor-targeted release, fluorescence-guided monitoring, and EZH2 suppression, providing a versatile platform for precise CRC therapy. These findings support its potential for enhanced drug delivery and real-time treatment monitoring.</p>

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Construction of a Controlled Drug Delivery and Optical Monitoring System for Colorectal Cancer via Natural Fiber Modification

  • 期刊论文

  • 发表日期：

    2025年3月28日

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  • Quan Cheng,
  • Huazhou Fu,
  • Yong Mao

摘要

Purpose

Colorectal cancer (CRC) is a leading digestive malignancy often diagnosed at advanced stages due to the absence of early biomarkers, resulting in poor prognosis. Effective drug delivery is crucial for improving outcomes. This study introduces FA-OHEC-APTES, a pH-responsive nano-drug delivery system, developed by modifying natural fibers (OHEC) with folic acid (FA) and 3-aminopropyltriethoxysilane (APTES) to enable targeted delivery, controlled release, and fluorescence tracking.

Methods

FA-OHEC-APTES was synthesized and characterized using FTIR, SEM, and nitrogen adsorption-desorption isotherms, confirming its porous nanoscale structure that facilitates drug loading and sustained release. Compound 1, a novel anti-CRC agent, was encapsulated to form FA-OHEC-APTES@1. Fluorescence spectroscopy evaluated pH-responsive drug release, while CCK-8 and qPCR assays assessed its therapeutic effects in HT29 colorectal cancer cells.

Results

FA-OHEC-APTES@1 exhibited pH-sensitive release, with 72.5% at pH 5.5 versus 35.8% at pH 7.4, aligning with the acidic tumor microenvironment. CCK-8 assays revealed dose-dependent inhibition of HT29 proliferation, with 70% viability reduction at 30 µM (P < 0.01). qPCR analysis showed 45% downregulation of EZH2, suggesting epigenetic modulation.

Conclusion

FA-OHEC-APTES@1 demonstrates acidic tumor-targeted release, fluorescence-guided monitoring, and EZH2 suppression, providing a versatile platform for precise CRC therapy. These findings support its potential for enhanced drug delivery and real-time treatment monitoring.