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Development of Domperidone Solid Lipid Nanoparticles: In Vitro and In Vivo Characterization.
AAPS PharmSciTech. 2018 May; 19(4):1712-1719.AP

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.

Authors+Show Affiliations

Department of Pharmaceutics, College of Pharmacy, King Saud University, P.O. Box 2457, Riyadh, 11451, Saudi Arabia. Department of Industrial Pharmacy, Faculty of Pharmacy, Assiut University, Assiut, Egypt.Department of Pharmaceutics, College of Pharmacy, King Saud University, P.O. Box 2457, Riyadh, 11451, Saudi Arabia.Department of Pharmaceutics, College of Pharmacy, King Saud University, P.O. Box 2457, Riyadh, 11451, Saudi Arabia.Department of Industrial Pharmacy, Faculty of Pharmacy, Assiut University, Assiut, Egypt. Department of Pharmaceutics and Pharmaceutical Technology, Faculty of Pharmacy, Mutah University, Mutah, Karak, 61710, Jordan.Department of Industrial Pharmacy, Faculty of Pharmacy, Assiut University, Assiut, Egypt.Faculty of Pharmacy, Delta University for Science and Technology, Gamasa City, Dakhlia, Egypt.Department of Pharmaceutics, College of Pharmacy, King Saud University, P.O. Box 2457, Riyadh, 11451, Saudi Arabia. faiyazs@fastmail.fm.

Pub Type(s)

Journal Article

Language

eng

PubMed ID

29532427

Citation

Shazly, Gamal A., et al. "Development of Domperidone Solid Lipid Nanoparticles: in Vitro and in Vivo Characterization." AAPS PharmSciTech, vol. 19, no. 4, 2018, pp. 1712-1719.
Shazly GA, Alshehri S, Ibrahim MA, et al. Development of Domperidone Solid Lipid Nanoparticles: In Vitro and In Vivo Characterization. AAPS PharmSciTech. 2018;19(4):1712-1719.
Shazly, G. A., Alshehri, S., Ibrahim, M. A., Tawfeek, H. M., Razik, J. A., Hassan, Y. A., & Shakeel, F. (2018). Development of Domperidone Solid Lipid Nanoparticles: In Vitro and In Vivo Characterization. AAPS PharmSciTech, 19(4), 1712-1719. https://doi.org/10.1208/s12249-018-0987-2
Shazly GA, et al. Development of Domperidone Solid Lipid Nanoparticles: in Vitro and in Vivo Characterization. AAPS PharmSciTech. 2018;19(4):1712-1719. PubMed PMID: 29532427.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Development of Domperidone Solid Lipid Nanoparticles: In Vitro and In Vivo Characterization. AU - Shazly,Gamal A, AU - Alshehri,Sultan, AU - Ibrahim,Mohamed A, AU - Tawfeek,Hesham M, AU - Razik,Jelan A, AU - Hassan,Yasser A, AU - Shakeel,Faiyaz, Y1 - 2018/03/12/ PY - 2018/01/24/received PY - 2018/02/28/accepted PY - 2018/3/14/pubmed PY - 2018/9/4/medline PY - 2018/3/14/entrez KW - bioavailability KW - dissolution KW - domperidone KW - pharmacokinetics KW - solid lipid nanoparticles SP - 1712 EP - 1719 JF - AAPS PharmSciTech JO - AAPS PharmSciTech VL - 19 IS - 4 N2 - 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. SN - 1530-9932 UR - https://www.unboundmedicine.com/medline/citation/29532427/Development_of_Domperidone_Solid_Lipid_Nanoparticles:_In_Vitro_and_In_Vivo_Characterization_ L2 - https://dx.doi.org/10.1208/s12249-018-0987-2 DB - PRIME DP - Unbound Medicine ER -