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Synthesis of Aptamer-PEI-g-PEG Modified Gold Nanoparticles Loaded with Doxorubicin for Targeted Drug Delivery
Published on: June 23, 2020
Targeted delivery of doxorubicin using a colorectal cancer-specific ssDNA aptamer
Wanming Li1, Hang Chen, Min Yu
1Department of Cell Biology, Key Laboratory of Cell Biology, Ministry of Public Health, China Medical University, Shenyang, 110001, China; Department of Cell Biology, Key Laboratory of Medical Cell Biology, Ministry of Education, China Medical University, Shenyang, 110001, China.
Abstract:
Targeted drug delivery is particularly important in cancer treatment because many antitumor drugs are nonspecific and highly toxic to both cancerous and normal cells. The L33 aptamer is a single-stranded DNA (ssDNA) sequence that has the ability to recognize human colorectal cancer (CRC) cell line HCT116 specifically. In this study, we demonstrated that the L33 aptamer can selectively internalize into target HCT116 cells via receptor-mediated endocytosis. Based on this finding, we developed an aptamer-based drug delivery system using L33 as the carrier of the antitumor drug doxorubicin (Dox). The L33-Dox complex exhibited specific and high affinity (Kd = 14.3 ± 2.2 nM) binding to HCT116 cells. The results of cytotoxicity assays revealed that the L33-Dox complex was capable of selectively delivering the drug to the target HCT116 cells and lowered the toxicity for nontarget CL187 cells. These findings indicate that the aptamer-based targeted drug delivery system has the potential to be used in clinical settings and may overcome drug resistance to a certain extent because high drug dosages can be directed toward target cells.
Insights
This study developed an aptamer-drug conjugate for targeted cancer therapy. The L33 aptamer delivers doxorubicin specifically to colorectal cancer cells, reducing toxicity to healthy cells.
Area of Science:
- Biotechnology
- Molecular Biology
- Cancer Research
Background:
- Antitumor drugs often lack specificity, leading to toxicity in both cancerous and normal cells.
- Targeted drug delivery systems are crucial for improving cancer treatment efficacy and reducing side effects.
- Aptamers, as single-stranded DNA (ssDNA) sequences, offer specific molecular recognition capabilities.
Purpose of the Study:
- To develop an aptamer-based targeted drug delivery system for colorectal cancer (CRC).
- To utilize the L33 aptamer for specific delivery of the chemotherapeutic agent doxorubicin (Dox) to CRC cells.
- To evaluate the efficacy and specificity of the aptamer-drug conjugate in vitro.
Main Methods:
- Development of an L33 aptamer-doxorubicin (Dox) complex.
- Assessment of the binding affinity and specificity of the L33-Dox complex to HCT116 CRC cells.
- Cytotoxicity assays using HCT116 and nontarget CL187 cells to evaluate selective drug delivery.
Main Results:
- The L33 aptamer selectively internalizes into HCT116 cells via receptor-mediated endocytosis.
- The L33-Dox complex demonstrated high-affinity binding (Kd = 14.3 ± 2.2 nM) to HCT116 cells.
- The L33-Dox complex selectively killed HCT116 cells while exhibiting reduced toxicity towards CL187 cells.
Conclusions:
- The L33 aptamer serves as an effective carrier for targeted doxorubicin delivery in colorectal cancer.
- This aptamer-based drug delivery system shows potential for clinical application in cancer therapy.
- Targeted delivery may help overcome drug resistance by concentrating high drug dosages at the tumor site.
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