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Updated: Jan 30, 2026

Activation and Conjugation of Soluble Polysaccharides using 1-Cyano-4-Dimethylaminopyridine Tetrafluoroborate CDAP
Published on: June 14, 2021
Boronate-crosslinked polysaccharide conjugates for pH-responsive and targeted drug delivery
Yu-Hui Zhang1, Ying-Ming Zhang2, Jie Yu3
1College of Science, Inner Mongolia Agricultural University, Hohhot 010018, P. R. China and Department of Chemistry, State Key Laboratory of Elemento-Organic Chemistry, Nankai University, Tianjin 300071, P. R. China. yuliu@nankai.edu.cn.
Researchers developed a pH-responsive polysaccharide conjugate using hyaluronic acid and the anticancer drug bortezomib. This targeted conjugate shows controlled drug release in acidic conditions, reducing toxicity and enhancing cancer cell inhibition.
Area of Science:
- Biomaterials Science
- Drug Delivery Systems
- Cancer Therapeutics
Background:
- Hyaluronic acid (HA) is a natural polysaccharide with potential in drug delivery due to its biocompatibility.
- Targeted drug delivery aims to increase therapeutic efficacy while minimizing systemic side effects.
- Bortezomib is a proteasome inhibitor used in cancer treatment, but its delivery can be challenging.
Purpose of the Study:
- To create a pH-responsive and targeted polysaccharide conjugate for improved bortezomib delivery.
- To evaluate the conjugate's drug release profile under acidic conditions.
- To assess the conjugate's cytotoxicity and anticancer efficacy compared to free bortezomib.
Main Methods:
- Fabrication of a conjugate using N-(2-aminoethyl)-gluconamide-grafted hyaluronic acid and bortezomib via a boronate linkage.
- Characterization of the conjugate's properties, including pH-responsiveness.
- In vitro evaluation of cytotoxicity and cancer cell inhibition using relevant cell lines.
Main Results:
- The fabricated polysaccharide conjugate demonstrated pH-responsive drug release, particularly under acidic conditions.
- The conjugate exhibited significantly lower cytotoxicity compared to free bortezomib.
- Enhanced inhibition effect on cancer cells was observed with the targeted conjugate.
Conclusions:
- The developed hyaluronic acid-based conjugate offers a promising platform for targeted and pH-responsive delivery of bortezomib.
- This approach enhances anticancer efficacy while reducing off-target toxicity.
- The study highlights the potential of polysaccharide conjugates in advanced cancer therapy.
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