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Folic Acid Functionalized Diallyl Trisulfide-Solid Lipid Nanoparticles for Targeting Triple Negative Breast Cancer
Anindita De1, Parikshit Roychowdhury2, Nihar Ranjan Bhuyan2
1College of Pharmacy, Gachon Institute of Pharmaceutical Science, Gachon University, Incheon 21936, Republic of Korea.
Abstract:
DATS (diallyl trisulfide), an anti-oxidant and cytotoxic chemical derived from the plant garlic, has been found to have potential therapeutic activity against triple-negative breast cancer (TNBC). Its hydrophobicity, short half-life, lack of target selectivity, and limited bioavailability at the tumor site limit its efficacy in treating TNBC. Overexpression of the Folate receptor on the surface of TNBC is a well-known target receptor for overcoming off-targeting, and lipid nanoparticles solve the limitations of limited bioavailability and short half-life. In order to overcome these constraints, we developed folic acid (FA)-conjugated DATS-SLNs in this research. The design of experiment (DoE) method was employed to optimize the FA-DATS-SLNs' nanoformulation, which resulted in a particle size of 168.2 ± 3.78 nm and a DATS entrapment of 71.91 ± 6.27%. The similarity index between MCF-7 and MDA-MB-231 cell lines demonstrates that FA-DATS-SLNs are more therapeutically efficacious in the treatment of aggravating TNBC. Higher cellular internalization and efficient Bcl2 protein downregulation support the hypothesis that functionalization of the FA on the surface of DATS-SLNs improves anticancer efficacy when compared with DATS and DATS-SLNs. FA-functionalized DATS-SLNs have demonstrated to be a promising therapeutic strategy for TNBC management.
Insights
Diallyl trisulfide (DATS) shows promise for triple-negative breast cancer (TNBC). Folic acid-conjugated DATS-SLNs enhance bioavailability and efficacy, offering a promising therapeutic strategy for TNBC management.
Area of Science:
- * Nanomedicine
- * Cancer Therapeutics
- * Drug Delivery Systems
Background:
- * Triple-negative breast cancer (TNBC) remains a challenging malignancy with limited targeted therapies.
- * Diallyl trisulfide (DATS), a garlic-derived compound, exhibits antioxidant and cytotoxic properties but suffers from poor bioavailability and targeting.
- * Folate receptor overexpression on TNBC cells presents a viable target for enhancing drug delivery and efficacy.
Purpose of the Study:
- * To develop and optimize folic acid (FA)-conjugated diallyl trisulfide-loaded solid lipid nanoparticles (DATS-SLNs) for improved TNBC treatment.
- * To investigate the therapeutic efficacy of FA-DATS-SLNs against TNBC cell lines.
- * To evaluate the role of FA functionalization in enhancing cellular uptake and anticancer activity.
Main Methods:
- * Design of Experiment (DoE) methodology was utilized for the optimization of FA-DATS-SLNs nanoformulation.
- * Particle size, DATS entrapment efficiency, and cellular internalization were characterized.
- * The effect of FA-DATS-SLNs on Bcl2 protein downregulation and therapeutic efficacy in TNBC cell lines (MCF-7 and MDA-MB-231) was assessed.
Main Results:
- * Optimized FA-DATS-SLNs achieved a particle size of 168.2 ± 3.78 nm with a DATS entrapment efficiency of 71.91 ± 6.27%.
- * FA-DATS-SLNs demonstrated superior therapeutic efficacy compared to DATS and DATS-SLNs in TNBC cell lines.
- * Enhanced cellular internalization and significant Bcl2 protein downregulation were observed with FA-functionalized DATS-SLNs.
Conclusions:
- * FA-functionalized DATS-SLNs represent a promising nanocarrier system for overcoming the limitations of DATS in TNBC therapy.
- * The targeted delivery facilitated by FA conjugation significantly improves the anticancer efficacy of DATS against TNBC.
- * This novel nanoformulation offers a potential therapeutic strategy for managing triple-negative breast cancer.
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