Preprint Article Version 1 Preserved in Portico This version is not peer-reviewed

Self-Micellizing Solid Dispersion of Thymoquinone with Enhanced Biopharmaceutical and Nephroprotective Effects

Shimul Halder
* ORCID logo ,
Sanjida Afrose
,
Manik Chandra Shill
,
Nahid Sharmin
,
Patricia Prova Mollick
,
Madhabi Lata Shuma
,
Md. Abdul Muhit
ORCID logo ,
S. M. Abdur Rahman
Version 1 : Received: 8 January 2023 / Approved: 10 January 2023 / Online: 10 January 2023 (03:09:17 CET)

How to cite: Halder, S.; Afrose, S.; Shill, M.C.; Sharmin, N.; Mollick, P.P.; Shuma, M.L.; Muhit, M.A.; Rahman, S.M.A. Self-Micellizing Solid Dispersion of Thymoquinone with Enhanced Biopharmaceutical and Nephroprotective Effects. Preprints 2023, 2023010170. https://doi.org/10.20944/preprints202301.0170.v1 Halder, S.; Afrose, S.; Shill, M.C.; Sharmin, N.; Mollick, P.P.; Shuma, M.L.; Muhit, M.A.; Rahman, S.M.A. Self-Micellizing Solid Dispersion of Thymoquinone with Enhanced Biopharmaceutical and Nephroprotective Effects. Preprints 2023, 2023010170. https://doi.org/10.20944/preprints202301.0170.v1

Abstract

The present study was designed to develop a self-micellizing solid dispersion (SMSD) containing Thymoquinone (TQM), a phytonutrient obtained from Nigella sativa seeds, aiming to improve its biopharmaceutical and nephroprotective functions. The apparent solubility of TQM in polymer solutions was used to choose an appropriate amphiphilic polymer that could be used to make an SMSD system. Based on the apparent solubility, Soluplus® was chosen as an appropriate carrier, and mixing with TQM, SMSD-TQM with different loadings of TQM (5–15%) was made by solvent evaporation and freeze-drying techniques, respectively, and the formulations were optimized. The optimized SMSD-TQM was evaluated in terms of particle size distribution, morphology, release characteristics, pharmacokinetic behavior, and nephroprotective effects in a rat model of acute kidney injury. SMSD-TQM significantly improved the dissolution characteristics (97.8%) of TQM in water within 60 min. Oral administration of SMSD-TQM in rats exhibited a 4.9-fold higher systemic exposure than crystalline TQM. In a cisplatin-induced (6 mg/kg, i.p.) acute kidney-damaged rat model, oral SMSD-TQM (10 mg/kg) improved the nephroprotective effects of TQM based on the results of kidney biomarkers and histological abnormalities. These findings suggest that SMSD-TQM might be efficacious in enhancing the nephroprotective effect of TQM by overcoming biopharmaceutical limitations.

Keywords

biopharmaceutical; nephroprotective; oral absorption; self-micellizing solid dispersion; thymoquinone.

Subject

Medicine and Pharmacology, Pharmacology and Toxicology

Copyright: This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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