Rathore, C.Upadhyay, N.Kaundal, R.Dwivedi, R. P.Rahatekar, Sameer S.John, A.Dua, KTambuwala, M. M.Jain, S.Chaudari, D.Negi, P.2020-04-292020-04-292020-01-31Rathore C, Upadhyay N, Kaundal R, et al., (2020) Enhanced oral bioavailability and hepatoprotective activity of thymoquinone in the form of phospholipidic nano-constructs. Expert Opinion on Drug Delivery, Volume 17, Issue 2, 2020, pp. 237-2531742-5247https://doi.org/10.1080/17425247.2020.1716728https://dspace.lib.cranfield.ac.uk/handle/1826/15416Background: 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.enAttribution-NonCommercial 4.0 Internationalhttp://creativecommons.org/licenses/by-nc/4.0/Thymoquinonebox-Behnken designlipid carriersmicroemulsifcationhepatotoxicitypharmacokineticsArticle