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

Date published

2020-01-31

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Taylor and Francis

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Article

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1742-5247

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Citation

Rathore 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. 237-253

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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Github

Keywords

Thymoquinone, box-Behnken design, lipid carriers, microemulsifcation, hepatotoxicity, pharmacokinetics

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Attribution-NonCommercial 4.0 International

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