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Development of Domperidone Solid Lipid Nanoparticles: In Vitro and In Vivo Characterization

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Abstract

Domperidone (DOP) is extensively applied orally in the management of nausea and vomiting. Upon oral administration, its bioavailability is very poor due to its poor solubility in alkaline media. Therefore, the aim of this work was to investigate DOP-loaded solid lipid nanoparticles (DOP-SLNs) in order to sustain its release pattern and to enhance oral bioavailability. DOP-SLNs were prepared using four different lipids. Prepared DOP-SLNs were characterized for “polydispersity index (PDI), particle size, zeta potential, % entrapment efficiency (% EE), and drug release behavior.” Differential scanning calorimetry (DSC) study was carried out to illustrate the physical form of DOP and excipients. The morphology of DOP-SLNs was confirmed by scanning electron microscopy (SEM). Pharmacokinetic study on optimized DOP-SLN in comparison to tablet was performed in rats. The “particle size, PDI, zeta potential, and % EE” of optimized formulation (F5) were recorded as 201.4 nm, 0.071, − 6.2 mV, and 66.3%, respectively. DSC thermograms suggested amorphous state of DOP in various SLNs. Surface morphology of SLNs using SEM suggested spherical shape of the nanoparticles within nanometer size range. In vitro release studies confirmed that all SLN formulations possessed a sustained release over a period of 12 h (51.3% from optimized formulation) in comparison with immediate release from conventional tablets (100% after 90 min). Pharmacokinetic study showed significant enhancement in oral absorption of DOP from optimized SLN in comparison with DOP tablet. The enhancement in relative bioavailability of DOP from optimized SLN was 2.62-fold in comparison with DOP tablet.

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Acknowledgements

“The authors would like to extend their sincere appreciation to the Deanship of Scientific Research at King Saud University for funding the work through research group project No. RGP-139.”

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Authors and Affiliations

  1. Department of Pharmaceutics, College of Pharmacy, King Saud University, P.O. Box 2457, Riyadh, 11451, Saudi Arabia

    Gamal A. Shazly, Sultan Alshehri, Mohamed A. Ibrahim & Faiyaz Shakeel

  2. Department of Industrial Pharmacy, Faculty of Pharmacy, Assiut University, Assiut, Egypt

    Gamal A. Shazly, Hesham M. Tawfeek & Jelan A. Razik

  3. Department of Pharmaceutics and Pharmaceutical Technology, Faculty of Pharmacy, Mutah University, Mutah, Karak, 61710, Jordan

    Hesham M. Tawfeek

  4. Faculty of Pharmacy, Delta University for Science and Technology, Gamasa City, Dakhlia, Egypt

    Yasser A. Hassan

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  1. Gamal A. Shazly
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Correspondence to Faiyaz Shakeel.

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Shazly, G.A., Alshehri, S., Ibrahim, M.A. et al. Development of Domperidone Solid Lipid Nanoparticles: In Vitro and In Vivo Characterization. AAPS PharmSciTech 19, 1712–1719 (2018). https://doi.org/10.1208/s12249-018-0987-2

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  • DOI: https://doi.org/10.1208/s12249-018-0987-2

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