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Transferrin Tethered Fluorescent Organic Nanoparticles for Receptor-Mediated Targeted Delivery of Paclitaxel to
Afreen Zaman1, Prasanta Kumar Das1
1School of Biological Sciences, Indian Association for the Cultivation of Science, Jadavpur, Kolkata, 700 032, India.
Abstract:
Cancer remains a critical global issue, marked by its high mortality rates. Despite achieving remarkable progress in cancer treatments, conventional chemotherapeutic drugs face numerous limitations. To this end, nanomaterial-based targeted drug delivery systems have emerged as a hope of promise. In this study, we report the design and development of transferrin (Tf) tethered naphthalene-diimide-based fluorescent organic nanoparticles (NDI-OH-Tf) for targeted delivery of paclitaxel to cancer cells with over expressed transferrin receptors (TfR). Spherical NDI-OH FONPs were fabricated through J-type of aggregation of NDI-OH amphiphiles in a 1:99 (v/v) DMSO-H2O mixture. These NDI-OH FONPs exhibited aggregation induced emission (AIE) at an emission wavelength of λem = 594 nm. The hydroxyl groups on the surface of the NDI-OH FONPs were conjugated with carboxyl groups of transferrin, forming NDI-OH-Tf FONPs. These NDI-OH-Tf FONPs were successfully used for targeted bioimaging and drug delivery to TfR+ cancer cells through ligand receptor interaction between transferrin and TfR. Notably, paclitaxel loaded NDI-OH-Tf exhibited ∼2.9-fold higher efficacy toward TfR+ cancer cells compared to normal cells and ∼3.3-fold higher cytotoxicity than free PTX due to transferrin mediated targeted accumulation of PTX in cancer cells.
Insights
Researchers developed transferrin-tethered fluorescent organic nanoparticles for targeted cancer drug delivery. These nanoparticles show enhanced paclitaxel efficacy in cancer cells overexpressing transferrin receptors, offering a promising approach for improved cancer treatment.
Area of Science:
- Nanotechnology
- Materials Science
- Biomedical Engineering
Background:
- Conventional chemotherapy faces limitations, including low efficacy and severe side effects.
- Nanomaterial-based drug delivery systems offer a promising alternative for targeted cancer therapy.
- Targeting overexpressed receptors on cancer cells is a key strategy for enhancing drug delivery.
Purpose of the Study:
- To design and develop transferrin (Tf) tethered naphthalene-diimide-based fluorescent organic nanoparticles (NDI-OH-Tf).
- To investigate the targeted delivery of paclitaxel (PTX) to cancer cells overexpressing transferrin receptors (TfR).
- To evaluate the efficacy and cytotoxicity of the developed nanoparticles for cancer treatment.
Main Methods:
- Fabrication of spherical NDI-OH fluorescent organic nanoparticles (FONPs) via J-type aggregation.
- Conjugation of transferrin to the hydroxyl groups on the FONP surface.
- Loading of paclitaxel into the NDI-OH-Tf FONPs.
- Evaluation of targeted bioimaging and drug delivery to TfR+ cancer cells.
Main Results:
- NDI-OH FONPs exhibited aggregation-induced emission (AIE) at λem = 594 nm.
- NDI-OH-Tf FONPs demonstrated successful targeted delivery to TfR+ cancer cells via ligand-receptor interaction.
- Paclitaxel-loaded NDI-OH-Tf showed significantly higher efficacy (~2.9-fold) and cytotoxicity (~3.3-fold) in TfR+ cancer cells compared to normal cells and free PTX.
Conclusions:
- Transferrin-mediated targeted delivery using NDI-OH-Tf FONPs is effective for cancer therapy.
- This approach enhances drug accumulation in cancer cells, leading to improved therapeutic outcomes.
- The developed nanoparticles hold potential for advanced cancer treatment strategies.
