Hypolipidemic Activity of Olive Oil-Based Nanostructured Lipid Carrier Containing Atorvastatin

Currently, hyperlipidemia is a growing health issue that is considered a risk factor for obesity. Controlling body weight and modifying life style in most of cases are not adequate and the condition requires medical treatment. Statin drugs (mainly Atorvastatin (ATO)), have been used broadly and for...

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Main Authors: Heba S. Elsewedy, Tamer M. Shehata, Mervt M. Almostafa, Wafaa E. Soliman
Format: Article
Language:English
Published: MDPI AG 2022-06-01
Series:Nanomaterials
Subjects:
Online Access:https://www.mdpi.com/2079-4991/12/13/2160
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author Heba S. Elsewedy
Tamer M. Shehata
Mervt M. Almostafa
Wafaa E. Soliman
author_facet Heba S. Elsewedy
Tamer M. Shehata
Mervt M. Almostafa
Wafaa E. Soliman
author_sort Heba S. Elsewedy
collection DOAJ
description Currently, hyperlipidemia is a growing health issue that is considered a risk factor for obesity. Controlling body weight and modifying life style in most of cases are not adequate and the condition requires medical treatment. Statin drugs (mainly Atorvastatin (ATO)), have been used broadly and for long time as medications for handling higher levels of lipid, especially bad cholesterol, which accordingly controls the prevalence of obesity. Still, the obstacle that stands in front of any formulation is the poor solubility of the drug. Low solubility of ATO came up with poor absorption as well as poor bioavailability. This paved the way for the present study, which aimed to exploit nanotechnology and develop certain nanolipid carriers that could accommodate hydrophobic drugs, such as ATO. Nanostructured lipid carrier (NLC) containing ATO was fabricated using olive oil. Olive oil is natural plant oil possessing confirmed hypolipidemic activity that would help in improving the efficacy of the formulation. Via applying the Quality by Design (QbD) approach, one NLC formula was selected to be optimized based on appropriate size and higher entrapment. Optimized ATO-NLC was scrutinized for zeta potential, in vitro study and kinetic profile. Moreover, stability testing and in vivo hypolipidemic behavior was conducted. The optimized NLC formulation seemed to show particle size (254.23 nm) with neutral zeta potential (−1.77 mV) and entrapment efficiency (69.56%). The formulation could be prolonged for 12 h and provided higher % of release (97.17%). Stability testing confirmed the role of modifying the surface of the formulation with PEG-DSPE in providing a highly stable formulation that could withstand three months storage in two altered conditions. Ultimately, optimized ATO-NLC could successfully lower total cholesterol level in rats induced with obesity and fed a high-fat diet. Remarkably, ATO-NLC prepared with olive oil, in addition to shielding its surface, would provide a stable formulation that holds up the synergistic action between olive oil and ATO.
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spelling doaj.art-9d40ac50f49546dea68e651d5ad5f50f2023-11-30T22:16:02ZengMDPI AGNanomaterials2079-49912022-06-011213216010.3390/nano12132160Hypolipidemic Activity of Olive Oil-Based Nanostructured Lipid Carrier Containing AtorvastatinHeba S. Elsewedy0Tamer M. Shehata1Mervt M. Almostafa2Wafaa E. Soliman3Al Bilad Bank Scholarly Chair for Food and Security in Saudi Arabia, The Deanship of Scientific Research, The Vice Presidency for Graduate Studies and Scientific Research, King Faisal University, Alhofuf 36362, Saudi ArabiaAl Bilad Bank Scholarly Chair for Food and Security in Saudi Arabia, The Deanship of Scientific Research, The Vice Presidency for Graduate Studies and Scientific Research, King Faisal University, Alhofuf 36362, Saudi ArabiaAl Bilad Bank Scholarly Chair for Food and Security in Saudi Arabia, The Deanship of Scientific Research, The Vice Presidency for Graduate Studies and Scientific Research, King Faisal University, Alhofuf 36362, Saudi ArabiaAl Bilad Bank Scholarly Chair for Food and Security in Saudi Arabia, The Deanship of Scientific Research, The Vice Presidency for Graduate Studies and Scientific Research, King Faisal University, Alhofuf 36362, Saudi ArabiaCurrently, hyperlipidemia is a growing health issue that is considered a risk factor for obesity. Controlling body weight and modifying life style in most of cases are not adequate and the condition requires medical treatment. Statin drugs (mainly Atorvastatin (ATO)), have been used broadly and for long time as medications for handling higher levels of lipid, especially bad cholesterol, which accordingly controls the prevalence of obesity. Still, the obstacle that stands in front of any formulation is the poor solubility of the drug. Low solubility of ATO came up with poor absorption as well as poor bioavailability. This paved the way for the present study, which aimed to exploit nanotechnology and develop certain nanolipid carriers that could accommodate hydrophobic drugs, such as ATO. Nanostructured lipid carrier (NLC) containing ATO was fabricated using olive oil. Olive oil is natural plant oil possessing confirmed hypolipidemic activity that would help in improving the efficacy of the formulation. Via applying the Quality by Design (QbD) approach, one NLC formula was selected to be optimized based on appropriate size and higher entrapment. Optimized ATO-NLC was scrutinized for zeta potential, in vitro study and kinetic profile. Moreover, stability testing and in vivo hypolipidemic behavior was conducted. The optimized NLC formulation seemed to show particle size (254.23 nm) with neutral zeta potential (−1.77 mV) and entrapment efficiency (69.56%). The formulation could be prolonged for 12 h and provided higher % of release (97.17%). Stability testing confirmed the role of modifying the surface of the formulation with PEG-DSPE in providing a highly stable formulation that could withstand three months storage in two altered conditions. Ultimately, optimized ATO-NLC could successfully lower total cholesterol level in rats induced with obesity and fed a high-fat diet. Remarkably, ATO-NLC prepared with olive oil, in addition to shielding its surface, would provide a stable formulation that holds up the synergistic action between olive oil and ATO.https://www.mdpi.com/2079-4991/12/13/2160hypolipidemicobesityolive oilatorvastatinnanostructured lipid carrier
spellingShingle Heba S. Elsewedy
Tamer M. Shehata
Mervt M. Almostafa
Wafaa E. Soliman
Hypolipidemic Activity of Olive Oil-Based Nanostructured Lipid Carrier Containing Atorvastatin
Nanomaterials
hypolipidemic
obesity
olive oil
atorvastatin
nanostructured lipid carrier
title Hypolipidemic Activity of Olive Oil-Based Nanostructured Lipid Carrier Containing Atorvastatin
title_full Hypolipidemic Activity of Olive Oil-Based Nanostructured Lipid Carrier Containing Atorvastatin
title_fullStr Hypolipidemic Activity of Olive Oil-Based Nanostructured Lipid Carrier Containing Atorvastatin
title_full_unstemmed Hypolipidemic Activity of Olive Oil-Based Nanostructured Lipid Carrier Containing Atorvastatin
title_short Hypolipidemic Activity of Olive Oil-Based Nanostructured Lipid Carrier Containing Atorvastatin
title_sort hypolipidemic activity of olive oil based nanostructured lipid carrier containing atorvastatin
topic hypolipidemic
obesity
olive oil
atorvastatin
nanostructured lipid carrier
url https://www.mdpi.com/2079-4991/12/13/2160
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AT mervtmalmostafa hypolipidemicactivityofoliveoilbasednanostructuredlipidcarriercontainingatorvastatin
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