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Freeze-dried lopinavir-loaded nanostructured lipid carriers for enhanced cellular uptake and bioavailability: statistical optimization, in vitro and in vivo evaluations.

Khan, Arshad Ali and Mudassir, Jahanzeb and Akhtar, Safia and Murugaiyah, Vikneswaran and Yusrida, Darwis (2019) Freeze-dried lopinavir-loaded nanostructured lipid carriers for enhanced cellular uptake and bioavailability: statistical optimization, in vitro and in vivo evaluations. Pharmaceutics, 11 (2). pp. 1-19. ISSN 1999-4923

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Abstract

Nanostructured lipid carriers (NLCs) loaded with lopinavir (LPV) were prepared by the high-shear homogenization method. The LPV-NLCs formulations were freeze-dried using trehalose as a cryoprotectant. In vitro release studies in simulated gastric fluid (pH 1.2) and simulated intestinal fluid (pH 6.8) showed a burst release. The optimized freeze-dried formulation (LPV-NLC-7-Tres) had a particle size (PS), polydispersity index (PdI), zeta potential (ZP) and % entrapment efficiency (%EE) of 286.8 ± 1.3 nm, 0.413 ± 0.017, −48.6 ± 0.89 mV and 88.31 ± 2.04%, respectively. The optimized formulation observed by transmission and scanning electron microscopes showed a spherical shape. Differential scanning calorimetry study revealed the absence of chemical interaction between the drug and lipids. In vitro cellular uptake study using Caco-2 cell line showed a higher LPV uptake from LPV-NLC-7-Tres formulation compared to the free LPV-suspension. The 6-month stability study showed a minimum rise of ~40 nm in PS, while no significant changes in PdI, ZP and drug content of the LPV-NLC-7-Tres formulation stored at 5 °C ± 3 °C. The bioavailability of LPV following oral administration of LPV-NLC-7-Tres in male Wistar rats was found 6.98-fold higher than the LPV-suspension. In conclusion, the nanostructure lipid carriers are potential carriers for improving the oral bioavailability of lopinavir.

Item Type: Article
Additional Information: Indexed by Web Of Science
Uncontrolled Keywords: Lopinavir; Lipid-based formulations; Cellular uptake; Factorial design
Subjects: Q Science > QP Physiology
Faculty/Division: Faculty of Engineering Technology
Depositing User: Mrs Norsaini Abdul Samat
Date Deposited: 10 Jun 2019 03:27
Last Modified: 10 Jun 2019 03:27
URI: http://umpir.ump.edu.my/id/eprint/24708
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