Merging Experimental Design and Nanotechnology for the Development of Optimized Simvastatin Spanlastics: A Promising Combined Strategy for Augmenting the Suppression of Various Human Cancer Cells
Simvastatin (SMV) is an antihyperlipidemic agent that has been investigated as a possible anti-cancer agent. An obstacle to malignant tumor therapy using drugs is the delivery of adequate levels to the cancer cells while minimizing side effects following their systemic administration. To circumvent...
Autores principales: | , , , , , , , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
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MDPI
2022
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9143367/ https://www.ncbi.nlm.nih.gov/pubmed/35631609 http://dx.doi.org/10.3390/pharmaceutics14051024 |
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author | Badr-Eldin, Shaimaa M. Aldawsari, Hibah M. Alhakamy, Nabil A. Fahmy, Usama A. Ahmed, Osama A. A. Neamatallah, Thikryat Tima, Singkome Almaghrabi, Raghad H. Alkudsi, Fayda M. Alamoudi, Asmaa A. Alzahrani, Amjad A. Kotta, Sabna Al-hejaili, Omar D. |
author_facet | Badr-Eldin, Shaimaa M. Aldawsari, Hibah M. Alhakamy, Nabil A. Fahmy, Usama A. Ahmed, Osama A. A. Neamatallah, Thikryat Tima, Singkome Almaghrabi, Raghad H. Alkudsi, Fayda M. Alamoudi, Asmaa A. Alzahrani, Amjad A. Kotta, Sabna Al-hejaili, Omar D. |
author_sort | Badr-Eldin, Shaimaa M. |
collection | PubMed |
description | Simvastatin (SMV) is an antihyperlipidemic agent that has been investigated as a possible anti-cancer agent. An obstacle to malignant tumor therapy using drugs is the delivery of adequate levels to the cancer cells while minimizing side effects following their systemic administration. To circumvent this challenge, the researchers directed towards the field of nanotechnology to benefit from the nano-size of the formulation in passively targeting the tumor cells. Thus, our study aimed at investigating the potential of a combined mixture–process variable design for optimization of SMV spanlastics (SMV-SPNs) with minimized particle size and maximized zeta potential to enhance the anticancer activity of the drug. The study investigated the effects of Span(®) 20 and Tween(®) 80 as mixture components and sonication time as a process variable on particle size, polydispersity index, and zeta potential as responses. SPNs were prepared using an ethanol injection method. Combining the predicted optimized variables’ levels is supposed to achieve the set goals with a desirability of 0.821. The optimized spanlastics exhibited a measured globule size of 128.50 nm, PDI of 0.329, and ZP of −29.11 mV. The percentage relative error between predicted responses and the observed ones were less than 5% for the three responses, indicating the optimization technique credibility. A significant improvement in the cytotoxicity of the optimized formulation against three different cancerous cell lines was observed in comparison with SMV. The inhibitory concentration (IC(50)) values of MCF-7, HCT-116, and HEPG2 were found to be 0.89, 0.39, and 0.06 μM at 24 h incubation. The enhanced cytotoxicity could be assigned to the possible improved permeation and preferential build-up within the cancerous cells by virtue of the minimized size. These findings imply that SMV-SPNs could be an ideal strategy to combat cancer. |
format | Online Article Text |
id | pubmed-9143367 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2022 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
spelling | pubmed-91433672022-05-29 Merging Experimental Design and Nanotechnology for the Development of Optimized Simvastatin Spanlastics: A Promising Combined Strategy for Augmenting the Suppression of Various Human Cancer Cells Badr-Eldin, Shaimaa M. Aldawsari, Hibah M. Alhakamy, Nabil A. Fahmy, Usama A. Ahmed, Osama A. A. Neamatallah, Thikryat Tima, Singkome Almaghrabi, Raghad H. Alkudsi, Fayda M. Alamoudi, Asmaa A. Alzahrani, Amjad A. Kotta, Sabna Al-hejaili, Omar D. Pharmaceutics Article Simvastatin (SMV) is an antihyperlipidemic agent that has been investigated as a possible anti-cancer agent. An obstacle to malignant tumor therapy using drugs is the delivery of adequate levels to the cancer cells while minimizing side effects following their systemic administration. To circumvent this challenge, the researchers directed towards the field of nanotechnology to benefit from the nano-size of the formulation in passively targeting the tumor cells. Thus, our study aimed at investigating the potential of a combined mixture–process variable design for optimization of SMV spanlastics (SMV-SPNs) with minimized particle size and maximized zeta potential to enhance the anticancer activity of the drug. The study investigated the effects of Span(®) 20 and Tween(®) 80 as mixture components and sonication time as a process variable on particle size, polydispersity index, and zeta potential as responses. SPNs were prepared using an ethanol injection method. Combining the predicted optimized variables’ levels is supposed to achieve the set goals with a desirability of 0.821. The optimized spanlastics exhibited a measured globule size of 128.50 nm, PDI of 0.329, and ZP of −29.11 mV. The percentage relative error between predicted responses and the observed ones were less than 5% for the three responses, indicating the optimization technique credibility. A significant improvement in the cytotoxicity of the optimized formulation against three different cancerous cell lines was observed in comparison with SMV. The inhibitory concentration (IC(50)) values of MCF-7, HCT-116, and HEPG2 were found to be 0.89, 0.39, and 0.06 μM at 24 h incubation. The enhanced cytotoxicity could be assigned to the possible improved permeation and preferential build-up within the cancerous cells by virtue of the minimized size. These findings imply that SMV-SPNs could be an ideal strategy to combat cancer. MDPI 2022-05-09 /pmc/articles/PMC9143367/ /pubmed/35631609 http://dx.doi.org/10.3390/pharmaceutics14051024 Text en © 2022 by the authors. https://creativecommons.org/licenses/by/4.0/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 (https://creativecommons.org/licenses/by/4.0/). |
spellingShingle | Article Badr-Eldin, Shaimaa M. Aldawsari, Hibah M. Alhakamy, Nabil A. Fahmy, Usama A. Ahmed, Osama A. A. Neamatallah, Thikryat Tima, Singkome Almaghrabi, Raghad H. Alkudsi, Fayda M. Alamoudi, Asmaa A. Alzahrani, Amjad A. Kotta, Sabna Al-hejaili, Omar D. Merging Experimental Design and Nanotechnology for the Development of Optimized Simvastatin Spanlastics: A Promising Combined Strategy for Augmenting the Suppression of Various Human Cancer Cells |
title | Merging Experimental Design and Nanotechnology for the Development of Optimized Simvastatin Spanlastics: A Promising Combined Strategy for Augmenting the Suppression of Various Human Cancer Cells |
title_full | Merging Experimental Design and Nanotechnology for the Development of Optimized Simvastatin Spanlastics: A Promising Combined Strategy for Augmenting the Suppression of Various Human Cancer Cells |
title_fullStr | Merging Experimental Design and Nanotechnology for the Development of Optimized Simvastatin Spanlastics: A Promising Combined Strategy for Augmenting the Suppression of Various Human Cancer Cells |
title_full_unstemmed | Merging Experimental Design and Nanotechnology for the Development of Optimized Simvastatin Spanlastics: A Promising Combined Strategy for Augmenting the Suppression of Various Human Cancer Cells |
title_short | Merging Experimental Design and Nanotechnology for the Development of Optimized Simvastatin Spanlastics: A Promising Combined Strategy for Augmenting the Suppression of Various Human Cancer Cells |
title_sort | merging experimental design and nanotechnology for the development of optimized simvastatin spanlastics: a promising combined strategy for augmenting the suppression of various human cancer cells |
topic | Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9143367/ https://www.ncbi.nlm.nih.gov/pubmed/35631609 http://dx.doi.org/10.3390/pharmaceutics14051024 |
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