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Uptake of New Lipid-coated Nanoparticles Containing Falcarindiol by Human Mesenchymal Stem Cells
Published on: February 9, 2019
Folate receptor targeted NIR cleavable liposomal delivery system augment penetration and therapeutic efficacy in
Yirivinti Hayagreeva Dinakar1, Archana Karole1, Shabi Parvez1
1Infectious Disease Biology Laboratory, Institute of Nano Science and Technology, Knowledge City, Sector 81, Mohali, Punjab 140306, India.
Background:
Liposomes are predominantly used sorts of nanocarriers for active a targeted delivery through surface functionalization using targeting ligand. The folate receptors are overexpressed in various cancers including breast cancer and because of its binding aptitude specifically to folate receptors, folic acid became the attractive ligand.
Methods:
In this research, we have developed a folate and Poly-l-Lysine conjugate and coated this conjugate onto the liposomes. The prepared liposomes were characterized using DLS, FTIR, NMR, SEM, TEM, XRD, AFM, stability and drug release studies. Furthermore, in vitro studies were carried out on FR overexpressed breast cancer cell line.
Results:
The FA-LUT-ABC-Lip have diameter of 183 ± 3.17 nm with positive surface charge +33.65 ± 3 mV and the drug release studies confirm the NIR responsive payload cleavage. The coated formulation (in presence of NIR light) effectively reduced the IC50 values and kills breast cancer cells through FR mediated internalization and accelerated drug release. Moreover, LUT Formulation shows anticancer effect due to significant inhibition of cell migration and proliferation by regulating VEGF expression and induced apoptosis through the caspase-3 up-regulation.
Conclusion:
It is evident from the in vitro studies that the formulation was found to be very effective and can be explored for triggered and targeted delivery of the substances through active targeting.
General Significance:
Combining receptor mediated drug delivery with triggered release aid in more amounts of drug reaching the target site and achieving enhanced therapeutic activity.
Insights
This study developed folate-functionalized liposomes for targeted breast cancer therapy. The targeted liposomes effectively deliver drugs to cancer cells, enhancing treatment efficacy through receptor-mediated internalization and triggered release.
Area of Science:
- Nanotechnology
- Biomedical Engineering
- Cancer Therapy
Background:
- Liposomes are key nanocarriers for targeted drug delivery via surface functionalization.
- Folate receptors are overexpressed in many cancers, making folic acid an attractive targeting ligand.
- Folic acid's specific binding to folate receptors facilitates targeted cancer therapy.
Purpose of the Study:
- To develop and characterize folate-conjugated liposomes for targeted delivery to folate receptor-overexpressing breast cancer cells.
- To investigate the in vitro efficacy of these targeted liposomes in killing cancer cells.
- To evaluate the potential for triggered drug release and enhanced therapeutic activity.
Main Methods:
- Preparation and characterization of folate and Poly-l-Lysine conjugated liposomes.
- Utilized techniques including DLS, FTIR, NMR, SEM, TEM, XRD, and AFM for comprehensive analysis.
- Conducted in vitro studies on breast cancer cell lines, including drug release and cell viability assays.
Main Results:
- FA-LUT-ABC-Liposomes exhibited a diameter of 183 nm and a positive surface charge of +33.65 mV.
- Near-infrared (NIR) light triggered payload cleavage, leading to reduced IC50 values and cancer cell death.
- The formulation demonstrated anticancer effects by inhibiting cell migration, regulating VEGF, and inducing apoptosis via caspase-3.
Conclusions:
- In vitro studies confirm the formulation's high efficacy for triggered and targeted drug delivery.
- The combination of receptor-mediated delivery and triggered release enhances drug accumulation at the target site.
- This approach holds significant potential for improving therapeutic outcomes in cancer treatment.

