Folic Acid Functionalized Diallyl Trisulfide-Solid Lipid Nanoparticles for Targeting Triple Negative Breast Cancer.

Anindita De, Parikshit Roychowdhury, Nihar Ranjan Bhuyan, Young Tag Ko, Sachin Kumar Singh, Kamal Dua, Gowthamarajan Kuppusamy
Author Information
  1. Anindita De: College of Pharmacy, Gachon Institute of Pharmaceutical Science, Gachon University, Incheon 21936, Republic of Korea. ORCID
  2. Parikshit Roychowdhury: Department of Pharmaceutical Chemistry, Himalayan Pharmacy Institute, Majitar 737136, East Sikkim, India.
  3. Nihar Ranjan Bhuyan: Department of Pharmaceutical Chemistry, Himalayan Pharmacy Institute, Majitar 737136, East Sikkim, India.
  4. Young Tag Ko: College of Pharmacy, Gachon Institute of Pharmaceutical Science, Gachon University, Incheon 21936, Republic of Korea. ORCID
  5. Sachin Kumar Singh: School of Pharmaceutical Sciences, Lovely Professional University, Phagwara 144411, Punjab, India. ORCID
  6. Kamal Dua: Faculty of Health, Australian Research Centre in Complementary & Integrative Medicine, University of Technology Sydney, Ultimo, NSW 2007, Australia. ORCID
  7. Gowthamarajan Kuppusamy: Department of Pharmaceutics, JSS College of Pharmacy, JSS Academy of Higher Education & Research, Ooty 643001, Tamil Nadu, India.

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.

Keywords

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Grants

  1. BT/PR23634/NER/95/786/2017./Department of Biotechnology

MeSH Term

Humans
Triple Negative Breast Neoplasms
Cell Line, Tumor
Apoptosis
Sulfides
Allyl Compounds
Nanoparticles

Chemicals

diallyl trisulfide
Lipid Nanoparticles
Sulfides
Allyl Compounds

Word Cloud

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