Enhanced oral bioavailability and hepatoprotective activity of thymoquinone in the form of phospholipidic nano-constructs.

Rathore, C; Upadhyay, N; Kaundal, R; Dwivedi, RP; Rahatekar, S; John, A; Dua, K; Tambuwala, MM; Jain, S; Chaudari, D; Negi, P

Enhanced oral bioavailability and hepatoprotective activity of thymoquinone in the form of phospholipidic nano-constructs.

Rathore, C Upadhyay, N Kaundal, R Dwivedi, RP Rahatekar, S John, A Dua, K

Tambuwala, MM Jain, S Chaudari, D Negi, P

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Publisher:: TAYLOR & FRANCIS LTD
Publication Type:: Journal Article
Citation:: Expert opinion on drug delivery, 2020, 17, (2), pp. 237-253
Issue Date:: 2020-02

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Field	Value	Language
dc.contributor.author	Rathore, C
dc.contributor.author	Upadhyay, N
dc.contributor.author	Kaundal, R
dc.contributor.author	Dwivedi, RP
dc.contributor.author	Rahatekar, S
dc.contributor.author	John, A
dc.contributor.author	Dua, K https://orcid.org/0000-0002-7507-1159
dc.contributor.author	Tambuwala, MM
dc.contributor.author	Jain, S
dc.contributor.author	Chaudari, D
dc.contributor.author	Negi, P
dc.date.accessioned	2020-08-17T04:25:22Z
dc.date.available	2020-08-17T04:25:22Z
dc.date.issued	2020-02
dc.identifier.citation	Expert opinion on drug delivery, 2020, 17, (2), pp. 237-253
dc.identifier.issn	1742-5247
dc.identifier.issn	1744-7593
dc.identifier.uri	http://hdl.handle.net/10453/142145
dc.description.abstract	Background: The poor biopharmaceutical properties of thymoquinone (TQ) obstruct its development as a hepatoprotective agent. To surmount the delivery challenges of TQ, phospholipid nanoconstructs (PNCs) were constructed.Method: PNCs were constructed employing microemulsification technique and systematic optimization by three-factor three level Box-Behnken design.Result: Optimized PNC composition exhibited nano size (<100 nm), spherical morphology, within acceptable range of polydispersity index (0.55), high drug entrapment efficiency (>90%), controlled drug release pattern, and neutral surface charge (zeta potential of -0.65 mV). After oral administration of a single dose of PNC, it showed a relative bioavailability of 386.03% vis-à-vis plain TQ suspension. Further, TQ-loaded PNC demonstrated significant enhanced hepato-protective effect vis-à-vis pure TQ suspension and silymarin, as evidenced by reduction in the ALP, ALT, AST, bilirubin, and albumin level and ratified by histopathological analysis.Conclusion: TQ-loaded PNCs can be efficient nano-platforms for the management of hepatic disorders and promising drug delivery systems to enhance oral bioavailability of this hydrophobic molecule.
dc.format	Print-Electronic
dc.language	eng
dc.publisher	TAYLOR & FRANCIS LTD
dc.relation.ispartof	Expert opinion on drug delivery
dc.relation.isbasedon	10.1080/17425247.2020.1716728
dc.rights	info:eu-repo/semantics/closedAccess
dc.subject	1115 Pharmacology and Pharmaceutical Sciences
dc.title	Enhanced oral bioavailability and hepatoprotective activity of thymoquinone in the form of phospholipidic nano-constructs.
dc.type	Journal Article
utslib.citation.volume	17
utslib.location.activity	England
utslib.for	1115 Pharmacology and Pharmaceutical Sciences
pubs.organisational-group	/University of Technology Sydney/Faculty of Health
pubs.organisational-group	/University of Technology Sydney/Faculty of Health/Graduate School of Health/GSH.Pharmacy
pubs.organisational-group	/University of Technology Sydney
pubs.organisational-group	/University of Technology Sydney/Faculty of Health/Graduate School of Health
utslib.copyright.status	closed_access	*
pubs.consider-herdc	false
dc.date.updated	2020-08-17T04:25:07Z
pubs.issue	2
pubs.publication-status	Published
pubs.volume	17
utslib.citation.issue	2

Abstract:

Background: The poor biopharmaceutical properties of thymoquinone (TQ) obstruct its development as a hepatoprotective agent. To surmount the delivery challenges of TQ, phospholipid nanoconstructs (PNCs) were constructed.Method: PNCs were constructed employing microemulsification technique and systematic optimization by three-factor three level Box-Behnken design.Result: Optimized PNC composition exhibited nano size (<100 nm), spherical morphology, within acceptable range of polydispersity index (0.55), high drug entrapment efficiency (>90%), controlled drug release pattern, and neutral surface charge (zeta potential of -0.65 mV). After oral administration of a single dose of PNC, it showed a relative bioavailability of 386.03% vis-à-vis plain TQ suspension. Further, TQ-loaded PNC demonstrated significant enhanced hepato-protective effect vis-à-vis pure TQ suspension and silymarin, as evidenced by reduction in the ALP, ALT, AST, bilirubin, and albumin level and ratified by histopathological analysis.Conclusion: TQ-loaded PNCs can be efficient nano-platforms for the management of hepatic disorders and promising drug delivery systems to enhance oral bioavailability of this hydrophobic molecule.

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http://hdl.handle.net/10453/142145