- Title
- Enhanced oral bioavailability and hepatoprotective activity of thymoquinone in the form of phospholipidic nano-constructs
- Creator
- Rathore, C.; Upadhyay, N.; Kaundal, R.; Dwivedi, R. P.; Rahatekar, S.; John, A.; Dua, K.; Tambuwala, Murtaza M.; Jain, S.; Chaudari, D.; Negi, P.
- Relation
- Expert Opinion on Drug Delivery Vol. 17, Issue 2, p. 237-253
- Publisher Link
- http://dx.doi.org/10.1080/17425247.2020.1716728
- Publisher
- Taylor & Francis
- Resource Type
- journal article
- Date
- 2020
- Description
- 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.
- Subject
- thymoquinone; box-behnken design; lipid carriers; microemulsifcation; hepatotoxicity; pharmacokinetics
- Identifier
- http://hdl.handle.net/1959.13/1463014
- Identifier
- uon:46617
- Identifier
- ISSN:1742-5247
- Language
- eng
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