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Pharmacokinetics and tissue distribution of hydrazinocurcumin in rats

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Abstract

Background

Curcumin, a natural polyphenol from Curcuma longa, is known to possess diversified pharmacological roles including anti-inflammatory, antioxidant, antiproliferative and antiangiogenic properties; however, its bioavailability is severely limited due to its poor solubility, poor absorption, rapid metabolism, and significant elimination. Hydrazinocurcumin (HZC), a novel analogue of curcumin has been reported to overcome the limitations of curcumin and also possesses multiple pharmacological activities. The present study aimed to evaluate the unexplored pharmacokinetic profile of this agent in experimental rats.

Methods

Drug formulations were administered to the experimental animals via oral, intravenous and intraperitoneal routes. Blood samples were collected at different pre-determined time intervals to determine the pharmacokinetic parameters. To understand the biodistribution profile of HCZ, tissue samples were isolated from different groups of Sprague–Dawley rats at different time points. The pharmacokinetic parameters of HZC were evaluated after administration through oral (100 mg/kg), intraperitoneal (100 mg/kg) and intravenous (10 mg/kg) routes.

Results

Significantly (p < 0.05) higher total AUC along with maximum concentration were evident with intraperitoneal administration when compared to the results of oral administration at a similar dose. In addition, shorter time to peak was observed with intraperitoneal administration. These results revealed a faster rate and longer duration of absorption with intraperitoneal administration, which further resulted in enhanced absolute bioavailability of HZC (29.17%) when compared to 5.1% upon oral dosing. The obtained data from the pharmacokinetic study indicated that HZC was instantaneously distributed and moderately eliminated from body fluids.

Conclusion

Based on the findings, it could be concluded that absorption of HZC is much higher via intraperitoneal route of administration compared to the oral administration.

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Acknowledgements

The authors are grateful to management for offering the requisite technical help to accomplish this study.

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Authors and Affiliations

  1. Department of Pharmaceutical Sciences, M. M. College of Pharmacy, M. M. Deemed To Be University, Mullana, Ambala, Haryana, India

    Satyavert, Sumeet Gupta, Meenakshi Dhanawat & Kavita Munjal

  2. School of Pharmacy, International Medical University, Bukit Jalil, 57000, Kuala Lumpur, Malaysia

    Hira Choudhury

  3. Department of Pharmaceutical Sciences, College of Pharmacy, Gulf Medical University, 4184, Ajman, United Arab Emirates

    Shery Jacob

  4. Department of Pharmaceutical Sciences, College of Clinical Pharmacy, King Faisal University, Al-Ahsa, 31982, Saudi Arabia

    Anroop B. Nair

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  1. Satyavert
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Contributions

S: conceptualization, data curation, formal analysis, investigation, methodology and writing—original draft preparation. SG: conceptualization, data curation, formal analysis, investigation, methodology and writing—review and editing. HC: formal analysis, investigation, methodology and writing—review and editing. SJ: formal analysis, investigation, methodology and writing—review and editing. ABN: formal analysis, investigation, methodology and writing—review and editing. All authors have read and agreed to the published version of the manuscript.

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Correspondence to Sumeet Gupta.

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Satyavert, Gupta, S., Choudhury, H. et al. Pharmacokinetics and tissue distribution of hydrazinocurcumin in rats. Pharmacol. Rep 73, 1734–1743 (2021). https://doi.org/10.1007/s43440-021-00312-5

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  • DOI: https://doi.org/10.1007/s43440-021-00312-5

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