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Stimuli-Responsive Aptamer-Drug Conjugates for Targeted Drug Delivery and Controlled Drug Release
Shanshan Zhu1,2, Huan Gao2,3, Wenyuan Li2,3
1The Key Laboratory of Biomedical Information Engineering of Ministry of Education, Xi'an Jiaotong University, Xi'an, 710049, P. R. China.
Advanced Healthcare Materials
|May 14, 2024
Summary
This study developed dual-targeted cancer therapy using stimuli-responsive aptamer-drug conjugates (srApDCs). This approach enhances drug delivery and release within tumor cells, significantly improving therapeutic efficacy for cancer treatment.
Area of Science:
- Biomedical Engineering
- Nanotechnology
- Cancer Therapeutics
Background:
- Chemotherapy efficacy is limited by inefficient anticancer agent delivery.
- Inefficient cellular internalization and intracellular drug release hinder cancer treatment.
- Current active targeting or tumor microenvironment (TME)-responsive strategies offer limited therapeutic improvement.
Purpose of the Study:
- To develop a dual-targeted strategy combining active targeting and TME-responsiveness for enhanced cancer therapy.
- To construct and evaluate stimuli-responsive aptamer-drug conjugates (srApDCs) for targeted drug delivery and controlled release.
- To investigate the potential of srApDCs to augment drug delivery efficiency and therapeutic outcomes.
Main Methods:
- Conjugation of a tumor-targeting aptamer (AS1411) with drugs using various stimuli-responsive linkers to create srApDCs.
- Evaluation of srApDCs for selective cellular uptake mediated by the aptamer.
- Assessment of drug release triggered by pathological cues within the TME.
- Experimental validation of enhanced therapeutic efficacy.
Main Results:
- Aptamer component selectively enhanced the uptake of srApDCs into tumor cells.
- Stimuli-responsive linkers facilitated drug payload release upon cleavage by TME-specific pathological cues.
- The dual-targeted approach led to a significant enhancement in therapeutic efficacy compared to individual strategies.
- Experimental data validated the design hypothesis for srApDCs.
Conclusions:
- Stimuli-responsive aptamer-drug conjugates (srApDCs) represent a promising dual-targeted strategy for cancer therapy.
- This approach effectively improves drug delivery efficiency through enhanced cellular internalization and controlled intracellular release.
- The developed methodology offers a novel and potent approach for improving cancer treatment outcomes.
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