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

De, A; Roychowdhury, P; Bhuyan, NR; Ko, YT; Singh, SK; Dua, K; Kuppusamy, G

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

De, A Roychowdhury, P Bhuyan, NR Ko, YT Singh, SK Dua, K

Kuppusamy, G

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Publisher:: MDPI AG
Publication Type:: Journal Article
Citation:: Molecules, 28, (3), pp. 1393-1393

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Field	Value	Language
dc.contributor.author	De, A
dc.contributor.author	Roychowdhury, P
dc.contributor.author	Bhuyan, NR
dc.contributor.author	Ko, YT
dc.contributor.author	Singh, SK
dc.contributor.author	Dua, K https://orcid.org/0000-0002-7507-1159
dc.contributor.author	Kuppusamy, G
dc.date.accessioned	2023-02-03T13:01:33Z
dc.date.available	2023-02-03T13:01:33Z
dc.identifier.citation	Molecules, 28, (3), pp. 1393-1393
dc.identifier.issn	1420-3049
dc.identifier.uri	http://hdl.handle.net/10453/165892
dc.description.abstract	<jats:p>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.</jats:p>
dc.language	en
dc.publisher	MDPI AG
dc.relation.ispartof	Molecules
dc.relation.isbasedon	10.3390/molecules28031393
dc.rights	info:eu-repo/semantics/openAccess
dc.subject	0304 Medicinal and Biomolecular Chemistry, 0305 Organic Chemistry, 0307 Theoretical and Computational Chemistry
dc.subject.classification	Organic Chemistry
dc.title	Folic Acid Functionalized Diallyl Trisulfide–Solid Lipid Nanoparticles for Targeting Triple Negative Breast Cancer
dc.type	Journal Article
utslib.citation.volume	28
utslib.for	0304 Medicinal and Biomolecular Chemistry
utslib.for	0305 Organic Chemistry
utslib.for	0307 Theoretical and Computational Chemistry
pubs.organisational-group	/University of Technology Sydney
pubs.organisational-group	/University of Technology Sydney/Faculty of Health
pubs.organisational-group	/University of Technology Sydney/Faculty of Health/Graduate School of Health
pubs.organisational-group	/University of Technology Sydney/Faculty of Health/Graduate School of Health/GSH.Pharmacy
utslib.copyright.status	open_access	*
dc.date.updated	2023-02-03T13:01:28Z
pubs.issue	3
pubs.publication-status	Published online
pubs.volume	28
utslib.citation.issue	3

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.

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http://hdl.handle.net/10453/165892