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

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...

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Main Authors:	Khan, Arshad Ali, Mudassir, Jahanzeb, Akhtar, Safia, Murugaiyah, Vikneswaran, Yusrida, Darwis
Format:	Article
Language:	English
Published:	MDPI 2019
Subjects:	QP Physiology
Online Access:	http://umpir.ump.edu.my/id/eprint/24708/ http://umpir.ump.edu.my/id/eprint/24708/ http://umpir.ump.edu.my/id/eprint/24708/ http://umpir.ump.edu.my/id/eprint/24708/1/Freeze-Dried%20Lopinavir-Loaded%20Nanostructured%20Lipid%20Carriers%20for%20Enhanced%20Cellular.pdf

id	ump-24708
recordtype	eprints
spelling	ump-247082019-06-10T03:27:51Z http://umpir.ump.edu.my/id/eprint/24708/ Freeze-dried lopinavir-loaded nanostructured lipid carriers for enhanced cellular uptake and bioavailability: statistical optimization, in vitro and in vivo evaluations. Khan, Arshad Ali Mudassir, Jahanzeb Akhtar, Safia Murugaiyah, Vikneswaran Yusrida, Darwis QP Physiology 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. MDPI 2019-02-25 Article PeerReviewed pdf en http://umpir.ump.edu.my/id/eprint/24708/1/Freeze-Dried%20Lopinavir-Loaded%20Nanostructured%20Lipid%20Carriers%20for%20Enhanced%20Cellular.pdf 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 https://doi.org/10.3390/pharmaceutics11020097 https://doi.org/10.3390/pharmaceutics11020097
repository_type	Digital Repository
institution_category	Local University
institution	Universiti Malaysia Pahang
building	UMP Institutional Repository
collection	Online Access
language	English
topic	QP Physiology
spellingShingle	QP Physiology Khan, Arshad Ali Mudassir, Jahanzeb Akhtar, Safia Murugaiyah, Vikneswaran Yusrida, Darwis Freeze-dried lopinavir-loaded nanostructured lipid carriers for enhanced cellular uptake and bioavailability: statistical optimization, in vitro and in vivo evaluations.
description	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.
format	Article
author	Khan, Arshad Ali Mudassir, Jahanzeb Akhtar, Safia Murugaiyah, Vikneswaran Yusrida, Darwis
author_facet	Khan, Arshad Ali Mudassir, Jahanzeb Akhtar, Safia Murugaiyah, Vikneswaran Yusrida, Darwis
author_sort	Khan, Arshad Ali
title	Freeze-dried lopinavir-loaded nanostructured lipid carriers for enhanced cellular uptake and bioavailability: statistical optimization, in vitro and in vivo evaluations.
title_short	Freeze-dried lopinavir-loaded nanostructured lipid carriers for enhanced cellular uptake and bioavailability: statistical optimization, in vitro and in vivo evaluations.
title_full	Freeze-dried lopinavir-loaded nanostructured lipid carriers for enhanced cellular uptake and bioavailability: statistical optimization, in vitro and in vivo evaluations.
title_fullStr	Freeze-dried lopinavir-loaded nanostructured lipid carriers for enhanced cellular uptake and bioavailability: statistical optimization, in vitro and in vivo evaluations.
title_full_unstemmed	Freeze-dried lopinavir-loaded nanostructured lipid carriers for enhanced cellular uptake and bioavailability: statistical optimization, in vitro and in vivo evaluations.
title_sort	freeze-dried lopinavir-loaded nanostructured lipid carriers for enhanced cellular uptake and bioavailability: statistical optimization, in vitro and in vivo evaluations.
publisher	MDPI
publishDate	2019
url	http://umpir.ump.edu.my/id/eprint/24708/ http://umpir.ump.edu.my/id/eprint/24708/ http://umpir.ump.edu.my/id/eprint/24708/ http://umpir.ump.edu.my/id/eprint/24708/1/Freeze-Dried%20Lopinavir-Loaded%20Nanostructured%20Lipid%20Carriers%20for%20Enhanced%20Cellular.pdf
first_indexed	2023-09-18T22:37:33Z
last_indexed	2023-09-18T22:37:33Z
_version_	1777416697330794496

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

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