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Efficient pH-Responsive Nano-Drug Delivery System Based on Dynamic Boronic Acid/Ester Transformation
Weijun Chen1, Wanxuan Xie2, Guangkuo Zhao2
1Department of Child Health Care, Children's Hospital, Zhejiang University School of Medicine, National Clinical Research Center for Child Health, Hangzhou 310052, China.
Molecules (Basel, Switzerland)
|June 10, 2023
Summary
This study introduces a novel pH-responsive nanoparticle system for chemotherapy delivery. The system enhances drug accumulation in tumors, improving efficacy and reducing systemic toxicity for cancer treatment.
Area of Science:
- Biomaterials Science
- Nanotechnology
- Cancer Therapeutics
Background:
- Traditional chemotherapy exhibits poor tumor selectivity, causing insufficient drug accumulation and significant systemic toxicity.
- Developing targeted drug delivery systems is crucial for enhancing cancer treatment efficacy and patient outcomes.
Purpose of the Study:
- To design and evaluate a boronic acid/ester-based pH-responsive nano-drug delivery system for improved cancer therapy.
- To target the acidic tumor microenvironment for enhanced drug accumulation and reduced systemic side effects.
Main Methods:
- Synthesized hydrophobic polyesters with phenylboronic acid groups (PBA-PAL) and hydrophilic PEGs (mPEG-DA).
- Formed amphiphilic structures via phenylboronic ester linkages, self-assembling into paclitaxel (PTX)-loaded nanoparticles (PTX/PBA NPs) using nanoprecipitation.
- Evaluated drug encapsulation efficiency, pH-triggered drug release, and in vitro/in vivo anticancer activity.
Main Results:
- PTX/PBA NPs demonstrated high drug encapsulation efficiency and pH-responsive drug release.
- In vitro and in vivo studies showed improved pharmacokinetics, potent anticancer activity, and low systemic toxicity.
- The nano-drug delivery system effectively targeted the acidic tumor microenvironment.
Conclusions:
- The developed boronic acid/ester-based pH-responsive nano-drug delivery system shows significant potential for enhancing chemotherapy efficacy.
- This system offers improved tumor targeting and reduced systemic toxicity, suggesting promising clinical applications in cancer treatment.
