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Fattigation-platform nanoparticles using apo-transferrin stearic acid as a core for receptor-oriented cancer
Hardik H Amin1, Nilesh M Meghani1, Chulhun Park1
1Bioavailability Control Laboratory, College of Pharmacy and Institute of Pharmaceutical Science and Technology, Ajou University, Suwon 16499, Republic of Korea.
Abstract:
A major hurdle in cancer treatment is the precise targeting of drugs to the cancer site. As many cancer cells overexpress the transferrin receptor (TfR), the transferrin (Tf)-TfR interaction is widely exploited to target cancer cells. In this study, novel amphiphilic apo-Tf stearic acid (TfS) conjugates were prepared and characterized by Fourier transform infrared (FTIR) spectroscopy, matrix-assisted laser desorption/ionization-time of flight (MALDI-TOF) mass spectrometry, and trinitrobenzenesulfonic acid (TNBS) assay. The prepared TfS conjugates were readily self-assembled in water to form nanoparticles (NPs), consisting of TfS as a core of NPs, whose sizes and zeta potentials were determined by scanning electron microscopy (SEM), transmission electron microscopy (TEM), and a particle size analyzer. Hydrophilic water-soluble doxorubicin (DOX) was chosen as a model drug. DOX-loaded TfS NPs (NP+DOX), prepared by the adsorption of DOX on the NP surface via the incubation method, were analyzed for their cell targeting and killing efficiencies in TfR-overexpressing A549 and HCT116 cell lines by MTT assay, confocal microscopy, and fluorescence assisted cell sorting (flow cytometry). The data showed that NP+DOX exhibited improved cancer cell targeting and killing properties compared to that reported for free DOX. Further, the cytotoxic efficiency of NP+DOX was comparable to that of PEGylated liposomal product, Doxil®, while its cellular uptake was higher than that of Doxil®. Thus, this novel receptor-based TfS NP drug delivery system has great potential to target TfR-overexpressing cancer cells without off-target effects.
Insights
Novel transferrin-based nanoparticles (NPs) effectively target cancer cells overexpressing the transferrin receptor (TfR). These NPs loaded with doxorubicin (DOX) show enhanced cancer cell killing and uptake compared to free DOX and Doxil®.
Area of Science:
- Biomaterials Science
- Nanotechnology
- Cancer Therapeutics
Background:
- Targeting cancer cells precisely remains a challenge in chemotherapy.
- The transferrin receptor (TfR) is overexpressed on many cancer cells, making it a viable target.
- Developing effective drug delivery systems is crucial for improving cancer treatment outcomes.
Purpose of the Study:
- To create novel amphiphilic apo-transferrin stearic acid (TfS) conjugates for nanoparticle (NP) formation.
- To evaluate the potential of TfS NPs as a drug delivery system for targeting TfR-overexpressing cancer cells.
- To assess the efficacy of doxorubicin (DOX)-loaded TfS NPs (NP+DOX) in vitro.
Main Methods:
- Synthesis and characterization of TfS conjugates using FTIR, MALDI-TOF, and TNBS assay.
- Formation and characterization of NPs using SEM, TEM, and particle size analysis.
- In vitro evaluation of NP+DOX targeting and cytotoxicity in A549 and HCT116 cells via MTT assay, confocal microscopy, and flow cytometry.
Main Results:
- TfS conjugates self-assembled into stable NPs with determined sizes and zeta potentials.
- NP+DOX demonstrated superior cancer cell targeting and killing efficiencies compared to free DOX.
- NP+DOX exhibited comparable cytotoxic efficiency to Doxil® but with higher cellular uptake.
Conclusions:
- Novel TfS NPs represent a promising drug delivery platform for targeting TfR-overexpressing cancer cells.
- This system offers potential for improved cancer therapy with reduced off-target effects.
- The TfS NP system shows significant potential in advancing targeted cancer treatment strategies.
