Self-nanoemulsifying drug delivery system (SNEDDS) mediated improved oral bioavailability of thymoquinone: optimization, characterization, pharmacokinetic, and hepatotoxicity studies

Rathore, C; Hemrajani, C; Sharma, AK; Gupta, PK; Jha, NK; Aljabali, AAA; Gupta, G; Singh, SK; Yang, J-C; Dwivedi, RP; Dua, K; Chellappan, DK; Negi, P; Tambuwala, MM

Self-nanoemulsifying drug delivery system (SNEDDS) mediated improved oral bioavailability of thymoquinone: optimization, characterization, pharmacokinetic, and hepatotoxicity studies

Rathore, C Hemrajani, C Sharma, AK Gupta, PK Jha, NK Aljabali, AAA Gupta, G Singh, SK Yang, J-C Dwivedi, RP Dua, K

Chellappan, DK Negi, P Tambuwala, MM

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Publisher:: Springer Science and Business Media LLC
Publication Type:: Journal Article
Citation:: Drug Delivery and Translational Research

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Field	Value	Language
dc.contributor.author	Rathore, C
dc.contributor.author	Hemrajani, C
dc.contributor.author	Sharma, AK
dc.contributor.author	Gupta, PK
dc.contributor.author	Jha, NK
dc.contributor.author	Aljabali, AAA
dc.contributor.author	Gupta, G
dc.contributor.author	Singh, SK
dc.contributor.author	Yang, J-C
dc.contributor.author	Dwivedi, RP
dc.contributor.author	Dua, K https://orcid.org/0000-0002-7507-1159
dc.contributor.author	Chellappan, DK
dc.contributor.author	Negi, P
dc.contributor.author	Tambuwala, MM
dc.date.accessioned	2022-07-14T08:23:48Z
dc.date.available	2022-07-14T08:23:48Z
dc.identifier.citation	Drug Delivery and Translational Research
dc.identifier.issn	2190-393X
dc.identifier.issn	2190-3948
dc.identifier.uri	http://hdl.handle.net/10453/158925
dc.description.abstract	<jats:title>Abstract</jats:title><jats:p>Thymoquinone (TQ) is an antioxidant, anti-inflammatory, and hepatoprotective compound obtained from the black seed oil of <jats:italic>Nigella sativa</jats:italic>. However, high hydrophobicity, instability at higher pH levels, photosensitivity, and low oral bioavailability hinder its delivery to the target tissues. A self-nanoemulsifying drug delivery system (SNEDDS) was fabricated using the microemulsification technique to address these issues. Its physicochemical properties, thermodynamic stability studies, drug release kinetics, in vivo pharmacokinetics, and hepatoprotective activity were evaluated. The droplet size was in the nano-range (< 90 nm). Zeta potential was measured to be −11.35 mV, signifying the high stability of the oil droplets. In vivo pharmacokinetic evaluation showed a fourfold increase in the bioavailability of TQ-SNEDDS over pure TQ. Furthermore, in a PCM-induced animal model, TQ-SNEDDS demonstrated significant (<jats:italic>p</jats:italic> < 0.05) hepatoprotective activity compared to pure TQ and silymarin. Reduction in liver biomarker enzymes and histopathological examinations of liver sections further supported the results. In this study, SNEDDS was demonstrated to be an improved oral delivery method for TQ, since it potentiates hepatotoxicity and enhances bioavailability.</jats:p> <jats:p><jats:bold>Graphical abstract</jats:bold></jats:p>
dc.language	en
dc.publisher	Springer Science and Business Media LLC
dc.relation.ispartof	Drug Delivery and Translational Research
dc.relation.isbasedon	10.1007/s13346-022-01193-8
dc.rights	info:eu-repo/semantics/closedAccess
dc.subject	1115 Pharmacology and Pharmaceutical Sciences
dc.title	Self-nanoemulsifying drug delivery system (SNEDDS) mediated improved oral bioavailability of thymoquinone: optimization, characterization, pharmacokinetic, and hepatotoxicity studies
dc.type	Journal Article
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	closed_access	*
dc.date.updated	2022-07-14T08:23:46Z
pubs.publication-status	Published online

Abstract:

AbstractThymoquinone (TQ) is an antioxidant, anti-inflammatory, and hepatoprotective compound obtained from the black seed oil of Nigella sativa. However, high hydrophobicity, instability at higher pH levels, photosensitivity, and low oral bioavailability hinder its delivery to the target tissues. A self-nanoemulsifying drug delivery system (SNEDDS) was fabricated using the microemulsification technique to address these issues. Its physicochemical properties, thermodynamic stability studies, drug release kinetics, in vivo pharmacokinetics, and hepatoprotective activity were evaluated. The droplet size was in the nano-range (< 90 nm). Zeta potential was measured to be −11.35 mV, signifying the high stability of the oil droplets. In vivo pharmacokinetic evaluation showed a fourfold increase in the bioavailability of TQ-SNEDDS over pure TQ. Furthermore, in a PCM-induced animal model, TQ-SNEDDS demonstrated significant (p < 0.05) hepatoprotective activity compared to pure TQ and silymarin. Reduction in liver biomarker enzymes and histopathological examinations of liver sections further supported the results. In this study, SNEDDS was demonstrated to be an improved oral delivery method for TQ, since it potentiates hepatotoxicity and enhances bioavailability. Graphical abstract

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http://hdl.handle.net/10453/158925