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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
Aptamer Functionalized Upconversion Nanotheranostic Agent With Nuclear Targeting as the Highly Localized
Xinyue Song1,2, Tao Yan1, Feng Tian1
1Shandong Provincial Key Laboratory of Detection Technology for Tumor Markers, College of Chemistry and Chemical Engineering, Linyi University, Shandong, China.
Abstract:
As a widely used anticancer drug, doxorubicin (DOX) could induce cell death mainly via interfering with DNA activity; thus, DOX could perform therapeutic effects mainly in the cell nucleus. However, most of the reported drug delivery systems lacked the well localization in the nucleus and released DOX molecules into the cytoplasm. Due to formidable barriers formed in the nuclear envelope, only around 1% of DOX could reach the nucleus and keep active. Therefore, DOX molecules were inevitably overloaded to achieve the desired therapeutic efficacy, which would induce serious side effects. Herein, we developed a highly localized drug nanocarrier for in situ release of DOX molecules to their action site where they could directly interfere with the DNA activity. In this work, we used cationic polymer-modified upconversion nanoparticles (UCNPs) as the luminescence core and gene carrier, while aptamers served as the DNA nanotrain to load DOX. Finally, the prepared nanotheranostic agent displayed good targetability, high cell apoptosis ratio (93.04%) with quite lower concentration than the LC50 of DOX, and obvious inhibition on tumor growth.
Insights
This study developed a novel nanocarrier for targeted delivery of doxorubicin (DOX) to cancer cell nuclei. The new system enhances DOX
Area of Science:
- Biomedical Engineering
- Nanotechnology
- Pharmacology
Background:
- Doxorubicin (DOX) is a crucial anticancer drug targeting DNA within the cell nucleus.
- Existing drug delivery systems struggle with nuclear localization, leading to suboptimal drug concentration and increased side effects.
- The nuclear envelope presents a significant barrier, limiting active DOX to approximately 1% in the nucleus.
Purpose of the Study:
- To develop a highly localized nanocarrier for in situ doxorubicin release directly at its nuclear DNA target.
- To improve therapeutic efficacy and reduce systemic toxicity of doxorubicin.
Main Methods:
- Utilized cationic polymer-modified upconversion nanoparticles (UCNPs) as a core for luminescence and gene delivery.
- Employed aptamers as a DNA nanotrain to load and transport doxorubicin (DOX).
- Characterized the nanotheranostic agent for its targeting, release, and therapeutic capabilities.
Main Results:
- The developed nanotheranostic agent demonstrated excellent targetability to cancer cells.
- Achieved a high cell apoptosis ratio of 93.04% at a significantly lower concentration than the doxorubicin LC50.
- Showed significant inhibition of tumor growth in experimental models.
Conclusions:
- The novel aptamer-functionalized UCNP nanocarrier enables precise nuclear delivery of doxorubicin.
- This targeted approach enhances anticancer efficacy while mitigating the side effects associated with conventional doxorubicin administration.
- The nanotheranostic agent holds promise for improved cancer treatment strategies.
