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A Flow Cytometry-Based Cell Surface Protein Binding Assay for Assessing Selectivity and Specificity of an Anticancer Aptamer
Published on: September 13, 2022
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Selective binding and controlled release of anticancer drugs by polyanionic cyclodextrins
Jian-Guang Cheng1, Hua-Jiang Yu1, Yong Chen1
1College of Chemistry, State Key Laboratory of Elemento-Organic Chemistry, Nankai University, PR China.
Bioorganic & Medicinal Chemistry
|March 28, 2018
Summary
New polyanionic cyclodextrins show high binding affinity for anticancer drugs, enabling pH-controlled drug release. These cyclodextrin derivatives are promising carriers for cancer therapeutics.
Area of Science:
- Supramolecular Chemistry
- Medicinal Chemistry
- Materials Science
Background:
- Cyclodextrins are widely used in drug delivery.
- Developing efficient carriers for anticancer drugs is crucial.
- Modifying cyclodextrins can enhance their drug-binding properties.
Purpose of the Study:
- To investigate the binding characteristics of novel polyanionic cyclodextrin derivatives with anticancer drugs.
- To evaluate the potential of these derivatives as drug delivery systems.
- To explore the pH-controlled release capabilities of the cyclodextrin-drug complexes.
Main Methods:
- Proton Nuclear Magnetic Resonance (¹H NMR)
- UV-Visible Spectroscopy
- Mass Spectrometry
- 2D NMR Spectroscopy
Main Results:
- Polyanionic cyclodextrins (H1-H2) exhibited high binding constants (2.6 × 10⁴–2.0 × 10⁵ M⁻¹) for irinotecan hydrochloride, topotecan hydrochloride, and doxorubicin hydrochloride.
- Binding affinities were significantly higher (50-1000 times) compared to native β-cyclodextrin.
- Demonstrated pH-controlled release, with efficient encapsulation at physiological pH and release at endosomal pH.
Conclusions:
- The investigated polyanionic cyclodextrins possess superior binding abilities for anticancer drugs.
- These cyclodextrin derivatives show potential as effective carriers for targeted cancer drug delivery.
- pH-responsive drug release mechanism enhances therapeutic potential by enabling release within cancer cells.
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