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Development of a Radiolabeled Folate-Mediated Drug Delivery System for Effective Delivery of Docetaxel
Oğuz Çetin1, Burcu Güngör1, Çiğdem İçhedef1
1Department of Nuclear Applications, Institute of Nuclear Sciences, Ege University, Izmir 35100, Turkey.
Abstract:
Many preclinical studies are carried out with the aim of developing new formulations for the effective delivery of taxane class drugs, one of the most important anticancer drugs used clinically today. In this study, a radiolabeled folate-mediated solid lipid magnetic nanoparticle (SLMNP) system was developed by loading superparamagnetic iron oxide nanoparticles (MNP) and docetaxel (DTX) into the solid lipid nanoparticles as a drug delivery system that will function both in cancer treatment and diagnosis. For this purpose, first, SLMNP was synthesized by the hot homogenization method, and the surface of the particles was modified with a folate derivative to carry the particles to tissues with folate receptors. The synthesized magnetic solid lipid nanoparticles were loaded with DTX, and then radiolabeling was carried out with technetium-99 m (99mTc-DTX-SLMNP). Structural characteristics of these nanoparticles were determined by characterization methods. According to the TEM images of MNPs, SLN, and SLMNPs, MNPs were observed between 25and 35 nm, SLNs between 400 and 500 nm, and SLMNPs between 350 and 450 nm. The drug entrapment efficiency of SLMNPs loaded with DTX was found to be 19%, and the percentage efficiency of radiolabeling was found to be 98.0 ± 2.0%. The biological behavior of this radiolabeled system was investigated in vitro and in vivo. Folate receptor-positive SKOV-3 and folate receptor-negative A549 cancer cell lines were studied. The IC50 values of DTX-SLMNP in SKOV-3 and A549 cells were 50.21 and 172.27 μM at 48 h, respectively. Gamma camera imaging studies of 99mTc-DTX-SLMNP and magnetically applied 99mTc-DTX-SLMNP compounds were performed on tumor-bearing CD-1 nude mice. The uptake in the folate receptor-positive tumor region was higher than that in the folate receptor negative tumor region. We proposed that the drug delivery system we prepared in this study be evaluated for preclinical studies of new drug carrier formulations of the taxane class of anticancer drugs.
Insights
This study developed a novel radiolabeled solid lipid magnetic nanoparticle (SLMNP) for targeted cancer therapy and diagnosis. The SLMNP system effectively delivered docetaxel (DTX) to folate receptor-positive tumors, showing promising preclinical results for taxane-based anticancer drug delivery.
Area of Science:
- Nanotechnology
- Oncology
- Radiopharmaceuticals
Background:
- Taxane-based chemotherapy is crucial for cancer treatment.
- Developing effective drug delivery systems for taxanes is an ongoing challenge.
- Targeted delivery can improve efficacy and reduce side effects.
Purpose of the Study:
- To develop a novel folate-mediated solid lipid magnetic nanoparticle (SLMNP) system for targeted delivery of docetaxel (DTX).
- To create a dual-purpose system for both cancer treatment and diagnosis.
- To evaluate the in vitro and in vivo performance of the radiolabeled SLMNP system.
Main Methods:
- Synthesis of SLMNPs using hot homogenization and surface modification with folate.
- Loading of docetaxel (DTX) and radiolabeling with technetium-99m (99mTc).
- Characterization of nanoparticle size, drug entrapment, and radiolabeling efficiency.
- In vitro cytotoxicity assays on folate receptor-positive (SKOV-3) and negative (A549) cancer cells.
- In vivo imaging studies in tumor-bearing mice using gamma camera and magnetic targeting.
Main Results:
- SLMNPs were successfully synthesized with sizes ranging from 350-450 nm.
- Drug entrapment efficiency was 19%, and radiolabeling efficiency reached 98.0 ± 2.0%.
- DTX-SLMNP showed significant cytotoxicity in SKOV-3 cells (IC50 = 50.21 μM) compared to A549 cells (IC50 = 172.27 μM).
- In vivo imaging demonstrated higher uptake in folate receptor-positive tumors, enhanced by magnetic application.
Conclusions:
- The developed folate-mediated SLMNP system is a promising platform for targeted docetaxel delivery in cancer therapy and diagnosis.
- The system exhibits enhanced tumor targeting and efficacy in preclinical models.
- Further evaluation in preclinical studies is warranted for taxane-class anticancer drug formulations.
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