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

Heba S Elsewedy; Tamer M Shehata; Mervt M Almostafa; Wafaa E Soliman

doi:10.3390/nano12132160

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

Nanomaterials (Basel). 2022 Jun 23;12(13):2160. doi: 10.3390/nano12132160.

Authors

Heba S Elsewedy^{1

2}, Tamer M Shehata^{1

2}, Mervt M Almostafa^{1

3}, Wafaa E Soliman^{1

4

5}

Affiliations

¹ Al 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 Arabia.
² Department of Pharmaceutical Sciences, College of Clinical Pharmacy, King Faisal University, Alhofuf 36362, Saudi Arabia.
³ Department of Chemistry, College of Science, King Faisal University, Alhofuf 36362, Saudi Arabia.
⁴ Department of Biomedical Sciences, College of Clinical Pharmacy, King Faisal University, Alhofuf 36362, Saudi Arabia.
⁵ Department of Microbiology and Immunology, Faculty of Pharmacy, Delta University for Science and Technology, Gamasa, Mansoura 11152, Egypt.

Abstract

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.

Keywords: atorvastatin; hypolipidemic; nanostructured lipid carrier; obesity; olive oil.

Grants and funding

Grant No., CHAIR54/Al Bilad Bank Scholarly Chair for Food Security in Saudi Arabia, the Deanship of Scientific Research, Vice Presidency for Graduate Studies and Scientific Research, King Faisal University, Saudi Arabia [Grant No. CHAIR54]. The APC was funded by the same "G