A kNGR Peptide-Tethered Lipid–Polymer Hybrid Nanocarrier-Based Synergistic Approach for Effective Tumor Therapy: Development, Characterization, Ex-Vivo, and In-Vivo Assessment

Gupta, M; Sharma, V; Sharma, K; Kumar, A; Sharma, A; Kazmi, I; Al-Abbasi, FA; Alzarea, SI; Afzal, O; Altamimi, ASA; Singh, SK; Gupta, G; Paudel, KR; Hansbro, PM; Dua, K

A kNGR Peptide-Tethered Lipid–Polymer Hybrid Nanocarrier-Based Synergistic Approach for Effective Tumor Therapy: Development, Characterization, Ex-Vivo, and In-Vivo Assessment

Gupta, M Sharma, V Sharma, K Kumar, A Sharma, A Kazmi, I Al-Abbasi, FA Alzarea, SI Afzal, O Altamimi, ASA Singh, SK Gupta, G Paudel, KR Hansbro, PM Dua, K

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Publisher:: MDPI AG
Publication Type:: Journal Article
Citation:: Pharmaceutics, 14, (7), pp. 1401-1401

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Field	Value	Language
dc.contributor.author	Gupta, M
dc.contributor.author	Sharma, V
dc.contributor.author	Sharma, K
dc.contributor.author	Kumar, A
dc.contributor.author	Sharma, A
dc.contributor.author	Kazmi, I
dc.contributor.author	Al-Abbasi, FA
dc.contributor.author	Alzarea, SI
dc.contributor.author	Afzal, O
dc.contributor.author	Altamimi, ASA
dc.contributor.author	Singh, SK
dc.contributor.author	Gupta, G
dc.contributor.author	Paudel, KR
dc.contributor.author	Hansbro, PM
dc.contributor.author	Dua, K https://orcid.org/0000-0002-7507-1159
dc.date.accessioned	2022-07-05T08:41:51Z
dc.date.available	2022-07-05T08:41:51Z
dc.identifier.citation	Pharmaceutics, 14, (7), pp. 1401-1401
dc.identifier.issn	1999-4923
dc.identifier.uri	http://hdl.handle.net/10453/158671
dc.description.abstract	<jats:p>The present study aims to design, develop and characterize kNGR (Asn-Gly-Arg) peptide-conjugated lipid–polymer-based nanoparticles for the target-specific delivery of anticancer bioactive(s), i.e., Paclitaxel (PTX). The kNGR-PEG-DSPE conjugate was synthesized and characterized by using spectral analysis. The dual-targeted PLGA–lecithin–PEG core-shell nanoparticles (PLNs-kNGR-NPs) were synthesized using a modified nanoprecipitation process, and their physiological properties were determined. The results support that, compared to other NPs, PLNs-kNGR-NPs are highly cytotoxic, owing to higher apoptosis and intracellular uptake. The significance of rational nanoparticle design for synergistic treatment is shown by the higher tumor volume inhibition percentage rate (59.7%), compared to other designed formulations in Balb/c mice in the HT-1080 tumor-induced model. The overall results indicate that the PLNs-kNGR-NPs-based hybrid lipid–polymer nanoparticles present the highest therapeutic efficacy against solid tumor overexpressing the CD13 receptors.</jats:p>
dc.language	en
dc.publisher	MDPI AG
dc.relation	http://purl.org/au-research/grants/nhmrc/1175134
dc.relation.ispartof	Pharmaceutics
dc.relation.isbasedon	10.3390/pharmaceutics14071401
dc.rights	info:eu-repo/semantics/openAccess
dc.subject	1115 Pharmacology and Pharmaceutical Sciences
dc.title	A kNGR Peptide-Tethered Lipid–Polymer Hybrid Nanocarrier-Based Synergistic Approach for Effective Tumor Therapy: Development, Characterization, Ex-Vivo, and In-Vivo Assessment
dc.type	Journal Article
utslib.citation.volume	14
utslib.for	1115 Pharmacology and Pharmaceutical Sciences
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	2022-07-05T08:41:48Z
pubs.issue	7
pubs.publication-status	Published online
pubs.volume	14
utslib.citation.issue	7

Abstract:

The present study aims to design, develop and characterize kNGR (Asn-Gly-Arg) peptide-conjugated lipid–polymer-based nanoparticles for the target-specific delivery of anticancer bioactive(s), i.e., Paclitaxel (PTX). The kNGR-PEG-DSPE conjugate was synthesized and characterized by using spectral analysis. The dual-targeted PLGA–lecithin–PEG core-shell nanoparticles (PLNs-kNGR-NPs) were synthesized using a modified nanoprecipitation process, and their physiological properties were determined. The results support that, compared to other NPs, PLNs-kNGR-NPs are highly cytotoxic, owing to higher apoptosis and intracellular uptake. The significance of rational nanoparticle design for synergistic treatment is shown by the higher tumor volume inhibition percentage rate (59.7%), compared to other designed formulations in Balb/c mice in the HT-1080 tumor-induced model. The overall results indicate that the PLNs-kNGR-NPs-based hybrid lipid–polymer nanoparticles present the highest therapeutic efficacy against solid tumor overexpressing the CD13 receptors.

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http://hdl.handle.net/10453/158671