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Externally Triggered Novel Rapid-Release Sonosensitive Folate-Modified Liposomes for Gemcitabine: Development and Characteristics
PURPOSE: To develop an externally triggered rapid-release targeted system for treating ovarian cancer, gemcitabine (GMC) was entrapped into sonosensitive (SoS) folate (Fo)-modified liposomes (LPs). METHODS: GMC-loaded LPs (GMC LPs), GMC-loaded Fo-targeted LPs (GMC-Fo LPs), and GMC-loaded Fo-targeted...
Autores principales: | , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
Dove
2021
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7850458/ https://www.ncbi.nlm.nih.gov/pubmed/33536754 http://dx.doi.org/10.2147/IJN.S266676 |
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author | Omar, Mahmoud M Hasan, Omiya Ali Zaki, Randa Mohammed Eleraky, Nermin E |
author_facet | Omar, Mahmoud M Hasan, Omiya Ali Zaki, Randa Mohammed Eleraky, Nermin E |
author_sort | Omar, Mahmoud M |
collection | PubMed |
description | PURPOSE: To develop an externally triggered rapid-release targeted system for treating ovarian cancer, gemcitabine (GMC) was entrapped into sonosensitive (SoS) folate (Fo)-modified liposomes (LPs). METHODS: GMC-loaded LPs (GMC LPs), GMC-loaded Fo-targeted LPs (GMC-Fo LPs), and GMC-loaded Fo-targeted SoS LPs (GMC-SoS Fo LPs) were prepared utilizing a film-hydration technique and evaluated based on particle size, ζ-potential, and percentage entrapped drug. Cellular uptake of the fluorescent delivery systems in Fo-expressing ovarian cancer cells was quantified using flow cytometry. Finally, tumor-targeting ability, in vivo evaluation, and pharmacokinetic studies were performed. RESULTS: GMC LPs, GMC-Fo LPs, and GMC-SoS Fo LPs were successfully prepared, with sizes of <120.3±2.4 nm, 39.7 mV ζ-potential, and 86.3%±1.84% entrapped drug. Cellular uptake of GMC-SoS Fo LPs improved 6.51-fold over GMC LPs (under ultrasonic irradiation — p<0.05). However, cellular uptake of GMC-Fo LPs improved just 1.24-fold over GMC LPs (p>0.05). Biodistribution study showed that of GMC concentration in tumors treated with GMC-SoS-Fo LPs (with ultrasound) improved 2.89-fold that of free GMC (p<0.05). In vivo, GMC-SoS Fo LPs showed the highest antiproliferative and antitumor action on ovarian cancer. CONCLUSION: These findings showed that externally triggered rapid-release SoS Fo-modified LPs are a promising system for delivering rapid-release drugs into tumors. |
format | Online Article Text |
id | pubmed-7850458 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2021 |
publisher | Dove |
record_format | MEDLINE/PubMed |
spelling | pubmed-78504582021-02-02 Externally Triggered Novel Rapid-Release Sonosensitive Folate-Modified Liposomes for Gemcitabine: Development and Characteristics Omar, Mahmoud M Hasan, Omiya Ali Zaki, Randa Mohammed Eleraky, Nermin E Int J Nanomedicine Original Research PURPOSE: To develop an externally triggered rapid-release targeted system for treating ovarian cancer, gemcitabine (GMC) was entrapped into sonosensitive (SoS) folate (Fo)-modified liposomes (LPs). METHODS: GMC-loaded LPs (GMC LPs), GMC-loaded Fo-targeted LPs (GMC-Fo LPs), and GMC-loaded Fo-targeted SoS LPs (GMC-SoS Fo LPs) were prepared utilizing a film-hydration technique and evaluated based on particle size, ζ-potential, and percentage entrapped drug. Cellular uptake of the fluorescent delivery systems in Fo-expressing ovarian cancer cells was quantified using flow cytometry. Finally, tumor-targeting ability, in vivo evaluation, and pharmacokinetic studies were performed. RESULTS: GMC LPs, GMC-Fo LPs, and GMC-SoS Fo LPs were successfully prepared, with sizes of <120.3±2.4 nm, 39.7 mV ζ-potential, and 86.3%±1.84% entrapped drug. Cellular uptake of GMC-SoS Fo LPs improved 6.51-fold over GMC LPs (under ultrasonic irradiation — p<0.05). However, cellular uptake of GMC-Fo LPs improved just 1.24-fold over GMC LPs (p>0.05). Biodistribution study showed that of GMC concentration in tumors treated with GMC-SoS-Fo LPs (with ultrasound) improved 2.89-fold that of free GMC (p<0.05). In vivo, GMC-SoS Fo LPs showed the highest antiproliferative and antitumor action on ovarian cancer. CONCLUSION: These findings showed that externally triggered rapid-release SoS Fo-modified LPs are a promising system for delivering rapid-release drugs into tumors. Dove 2021-01-28 /pmc/articles/PMC7850458/ /pubmed/33536754 http://dx.doi.org/10.2147/IJN.S266676 Text en © 2021 Omar et al. http://creativecommons.org/licenses/by-nc/3.0/ This work is published and licensed by Dove Medical Press Limited. The full terms of this license are available at https://www.dovepress.com/terms.php and incorporate the Creative Commons Attribution – Non Commercial (unported, v3.0) License (http://creativecommons.org/licenses/by-nc/3.0/). By accessing the work you hereby accept the Terms. Non-commercial uses of the work are permitted without any further permission from Dove Medical Press Limited, provided the work is properly attributed. For permission for commercial use of this work, please see paragraphs 4.2 and 5 of our Terms (https://www.dovepress.com/terms.php). |
spellingShingle | Original Research Omar, Mahmoud M Hasan, Omiya Ali Zaki, Randa Mohammed Eleraky, Nermin E Externally Triggered Novel Rapid-Release Sonosensitive Folate-Modified Liposomes for Gemcitabine: Development and Characteristics |
title | Externally Triggered Novel Rapid-Release Sonosensitive Folate-Modified Liposomes for Gemcitabine: Development and Characteristics |
title_full | Externally Triggered Novel Rapid-Release Sonosensitive Folate-Modified Liposomes for Gemcitabine: Development and Characteristics |
title_fullStr | Externally Triggered Novel Rapid-Release Sonosensitive Folate-Modified Liposomes for Gemcitabine: Development and Characteristics |
title_full_unstemmed | Externally Triggered Novel Rapid-Release Sonosensitive Folate-Modified Liposomes for Gemcitabine: Development and Characteristics |
title_short | Externally Triggered Novel Rapid-Release Sonosensitive Folate-Modified Liposomes for Gemcitabine: Development and Characteristics |
title_sort | externally triggered novel rapid-release sonosensitive folate-modified liposomes for gemcitabine: development and characteristics |
topic | Original Research |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7850458/ https://www.ncbi.nlm.nih.gov/pubmed/33536754 http://dx.doi.org/10.2147/IJN.S266676 |
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