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Comprehensive Study of Atorvastatin Nanostructured Lipid Carriers through Multivariate Conceptualization and Optimization

The aim of the current study is to establish a comprehensive experimental design for the screening and optimization of Atorvastatin-loaded nanostructured lipid carriers (AT-NLCs). Initially, combined D-optimal screening design was applied to find the most significant factors affecting AT-NLCs proper...

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Autores principales: Ghanem, Heba A., Nasr, Ali M., Hassan, Tamer H., Elkhoudary, Mahmoud M., Alshaman, Reem, Alattar, Abdullah, Gad, Shadeed
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2021
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7911144/
https://www.ncbi.nlm.nih.gov/pubmed/33525642
http://dx.doi.org/10.3390/pharmaceutics13020178
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author Ghanem, Heba A.
Nasr, Ali M.
Hassan, Tamer H.
Elkhoudary, Mahmoud M.
Alshaman, Reem
Alattar, Abdullah
Gad, Shadeed
author_facet Ghanem, Heba A.
Nasr, Ali M.
Hassan, Tamer H.
Elkhoudary, Mahmoud M.
Alshaman, Reem
Alattar, Abdullah
Gad, Shadeed
author_sort Ghanem, Heba A.
collection PubMed
description The aim of the current study is to establish a comprehensive experimental design for the screening and optimization of Atorvastatin-loaded nanostructured lipid carriers (AT-NLCs). Initially, combined D-optimal screening design was applied to find the most significant factors affecting AT-NLCs properties. The studied variables included mixtures of solid and liquid lipids, the solid/liquid lipid ratio, surfactant type and concentration, homogenization speed as well as sonication time. Then, the variables homogenization speed (A), the ratio of solid lipid/liquid lipid (B), and concentration of the surfactant (C) were optimized using a central composite design. Particle size, polydispersity index, zeta potential, and entrapment efficiency were chosen as dependent responses. The optimized AT-NLCs demonstrated a nanometric size (83.80 ± 1.13 nm), Polydispersity Index (0.38 ± 0.02), surface charge (−29.65 ± 0.65 mV), and high drug incorporation (93.1 ± 0.04%). Fourier Transform Infrared Spectroscopy (FTIR) analysis showed no chemical interaction between Atorvastatin and the lipid mixture. Differential Scanning Calorimetry (DSC) analysis of the AT-NLCs suggested the transformation of Atorvastatin crystal into an amorphous state. Administration of the optimized AT-NLCs led to a significant reduction (p < 0.001) in serum levels of rats’ total cholesterol, triglycerides, and low-density lipoproteins. This change was histologically validated by reducing the relevant steatosis of the liver.
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spelling pubmed-79111442021-02-28 Comprehensive Study of Atorvastatin Nanostructured Lipid Carriers through Multivariate Conceptualization and Optimization Ghanem, Heba A. Nasr, Ali M. Hassan, Tamer H. Elkhoudary, Mahmoud M. Alshaman, Reem Alattar, Abdullah Gad, Shadeed Pharmaceutics Article The aim of the current study is to establish a comprehensive experimental design for the screening and optimization of Atorvastatin-loaded nanostructured lipid carriers (AT-NLCs). Initially, combined D-optimal screening design was applied to find the most significant factors affecting AT-NLCs properties. The studied variables included mixtures of solid and liquid lipids, the solid/liquid lipid ratio, surfactant type and concentration, homogenization speed as well as sonication time. Then, the variables homogenization speed (A), the ratio of solid lipid/liquid lipid (B), and concentration of the surfactant (C) were optimized using a central composite design. Particle size, polydispersity index, zeta potential, and entrapment efficiency were chosen as dependent responses. The optimized AT-NLCs demonstrated a nanometric size (83.80 ± 1.13 nm), Polydispersity Index (0.38 ± 0.02), surface charge (−29.65 ± 0.65 mV), and high drug incorporation (93.1 ± 0.04%). Fourier Transform Infrared Spectroscopy (FTIR) analysis showed no chemical interaction between Atorvastatin and the lipid mixture. Differential Scanning Calorimetry (DSC) analysis of the AT-NLCs suggested the transformation of Atorvastatin crystal into an amorphous state. Administration of the optimized AT-NLCs led to a significant reduction (p < 0.001) in serum levels of rats’ total cholesterol, triglycerides, and low-density lipoproteins. This change was histologically validated by reducing the relevant steatosis of the liver. MDPI 2021-01-28 /pmc/articles/PMC7911144/ /pubmed/33525642 http://dx.doi.org/10.3390/pharmaceutics13020178 Text en © 2021 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Ghanem, Heba A.
Nasr, Ali M.
Hassan, Tamer H.
Elkhoudary, Mahmoud M.
Alshaman, Reem
Alattar, Abdullah
Gad, Shadeed
Comprehensive Study of Atorvastatin Nanostructured Lipid Carriers through Multivariate Conceptualization and Optimization
title Comprehensive Study of Atorvastatin Nanostructured Lipid Carriers through Multivariate Conceptualization and Optimization
title_full Comprehensive Study of Atorvastatin Nanostructured Lipid Carriers through Multivariate Conceptualization and Optimization
title_fullStr Comprehensive Study of Atorvastatin Nanostructured Lipid Carriers through Multivariate Conceptualization and Optimization
title_full_unstemmed Comprehensive Study of Atorvastatin Nanostructured Lipid Carriers through Multivariate Conceptualization and Optimization
title_short Comprehensive Study of Atorvastatin Nanostructured Lipid Carriers through Multivariate Conceptualization and Optimization
title_sort comprehensive study of atorvastatin nanostructured lipid carriers through multivariate conceptualization and optimization
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7911144/
https://www.ncbi.nlm.nih.gov/pubmed/33525642
http://dx.doi.org/10.3390/pharmaceutics13020178
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