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Quercetin-Loaded Mesoporous Silica Nanoparticle–Based Lyophilized Tablets for Enhanced Physicochemical Features and Dissolution Rate: Formulation, Optimization, and In Vitro Evaluation

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Abstract

Mesoporous silica nanoparticles (MSNPs) have been proposed as a potential approach for stabilizing the amorphous state of poorly water-soluble actives. This study aimed to improve the physiochemical characteristics of poorly water-soluble quercetin (QT) through a novel lyophilized formulation. Various parameters, including solvent polarity, QT-carrier mass ratio, and adsorption time, were studied to improve the loading of QT into MSNPs. The optimized loaded MSNPs were formulated into lyophilized tablets through a freeze-drying process using hydrophilic polyvinylpyrrolidone (PVP-K30) as a polymeric stabilizer and water-soluble sucrose as a cryoprotectant. The effect of PVP-K30 and sucrose on the particle size, disintegration time, friability, and time required to release 90% of QT were studied using 32 full factorial design. The optimized formula was characterized using different evaluating techniques; for instance, differential scanning calorimetry, X-ray diffractometry, Fourier transform infrared spectroscopy, drug content, moisture content, and saturation solubility. The analysis proved that QT was consistently kept in the nanosize range with a narrow size distribution. The loaded silica nanoparticles and the optimized formulation are in an amorphous state devoid of any chemical interaction with the silica matrix or the lyophilization excipients. The optimized formula also featured low friability (less than 1%), fast disintegration (< 30 s), and a pronounced enhancement in saturation solubility and dissolution rate. Briefly, we established that the lyophilized MSNPs-based tablet would be a potential strategy for improving the rate of dissolution and, ultimately, the bioavailability of the poorly water-soluble QT.

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Funding

This work was funded by the Deanship of Scientific Research at Jouf University under grant No (DSR-2021-01-03107).

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Authors and Affiliations

  1. Department of Pharmaceutics, College of Pharmacy, Jouf University, P.O. Box 2014, Sakaka, Saudi Arabia

    Mohammed Elmowafy, Nabil K. Alruwaili & Naveed Ahmad

  2. Department of Pharmaceutics and Pharmaceutical Technology, Faculty of Pharmacy (Boys), Al-Azhar University, Nasr City, Cairo, Egypt

    Abdulsalam M. Kassem & Mohamed F. Ibrahim

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  1. Mohammed Elmowafy
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Conception and design of the work, Abdulsalam M. Kassem and Mohamed F. Ibrahim; interpretation of data for the work, Abdulsalam M. Kassem and Mohammed Elmowafy; drafting the work, Abdulsalam M. Kassem and Nabil K. Alruwaili; revising the work critically for important intellectual content, Mohammed Elmowafy and Naveed Ahmad; final approval of the version to be published, Abdulsalam M. Kassem and Mohammed Elmowafy; and agreement to be accountable for all aspects of the work, Abdulsalam M. Kassem and Mohammed Elmowafy.

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Elmowafy, M., Alruwaili, N.K., Ahmad, N. et al. Quercetin-Loaded Mesoporous Silica Nanoparticle–Based Lyophilized Tablets for Enhanced Physicochemical Features and Dissolution Rate: Formulation, Optimization, and In Vitro Evaluation. AAPS PharmSciTech 24, 6 (2023). https://doi.org/10.1208/s12249-022-02464-w

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