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Ultrasound-Triggered Release of 5-Fluorouracil from Soy Lecithin Echogenic Liposomes

Colorectal cancer is the third most diagnosed cancer and the second leading cause of death. The use of 5-fluorouracil (5-FU) has been the major chemotherapeutic treatment for colorectal cancer patients. However, the efficacy of 5-FU is limited by drug resistance, and bone marrow toxicity through hig...

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Autores principales: Ezekiel, Charles Izuchukwu, Bapolisi, Alain Murhimalika, Walker, Roderick Bryan, Krause, Rui Werner Maçedo
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2021
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8229429/
https://www.ncbi.nlm.nih.gov/pubmed/34205990
http://dx.doi.org/10.3390/pharmaceutics13060821
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author Ezekiel, Charles Izuchukwu
Bapolisi, Alain Murhimalika
Walker, Roderick Bryan
Krause, Rui Werner Maçedo
author_facet Ezekiel, Charles Izuchukwu
Bapolisi, Alain Murhimalika
Walker, Roderick Bryan
Krause, Rui Werner Maçedo
author_sort Ezekiel, Charles Izuchukwu
collection PubMed
description Colorectal cancer is the third most diagnosed cancer and the second leading cause of death. The use of 5-fluorouracil (5-FU) has been the major chemotherapeutic treatment for colorectal cancer patients. However, the efficacy of 5-FU is limited by drug resistance, and bone marrow toxicity through high-level expression of thymidylate synthase, justifying the need for improvement of the therapeutic index. In this study, the effects of ultrasound on echogenic 5-FU encapsulated crude soy liposomes were investigated for their potential to address these challenges. Liposomes were prepared by thin-film hydration using crude soy lecithin and cholesterol. Argon gas was entrapped in the liposomes for sonosensitivity (that is, responsiveness to ultrasound). The nanoparticles were characterized for particle size and morphology. The physicochemical properties were also evaluated using differential scanning calorimetry, Fourier transform infrared and X-ray diffraction. The release profile of 5-FU was assessed with and without 20 kHz low-frequency ultrasound waves at various amplitudes and exposure times. The result reveal that 5-FU-loaded liposomes were spherical with an encapsulation efficiency of approximately 60%. Approximately 65% of 5-FU was released at the highest amplitude and exposure time was investigated. The results are encouraging for the stimulated and controlled release of 5-FU for the management of colorectal cancer.
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spelling pubmed-82294292021-06-26 Ultrasound-Triggered Release of 5-Fluorouracil from Soy Lecithin Echogenic Liposomes Ezekiel, Charles Izuchukwu Bapolisi, Alain Murhimalika Walker, Roderick Bryan Krause, Rui Werner Maçedo Pharmaceutics Article Colorectal cancer is the third most diagnosed cancer and the second leading cause of death. The use of 5-fluorouracil (5-FU) has been the major chemotherapeutic treatment for colorectal cancer patients. However, the efficacy of 5-FU is limited by drug resistance, and bone marrow toxicity through high-level expression of thymidylate synthase, justifying the need for improvement of the therapeutic index. In this study, the effects of ultrasound on echogenic 5-FU encapsulated crude soy liposomes were investigated for their potential to address these challenges. Liposomes were prepared by thin-film hydration using crude soy lecithin and cholesterol. Argon gas was entrapped in the liposomes for sonosensitivity (that is, responsiveness to ultrasound). The nanoparticles were characterized for particle size and morphology. The physicochemical properties were also evaluated using differential scanning calorimetry, Fourier transform infrared and X-ray diffraction. The release profile of 5-FU was assessed with and without 20 kHz low-frequency ultrasound waves at various amplitudes and exposure times. The result reveal that 5-FU-loaded liposomes were spherical with an encapsulation efficiency of approximately 60%. Approximately 65% of 5-FU was released at the highest amplitude and exposure time was investigated. The results are encouraging for the stimulated and controlled release of 5-FU for the management of colorectal cancer. MDPI 2021-06-01 /pmc/articles/PMC8229429/ /pubmed/34205990 http://dx.doi.org/10.3390/pharmaceutics13060821 Text en © 2021 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
Ezekiel, Charles Izuchukwu
Bapolisi, Alain Murhimalika
Walker, Roderick Bryan
Krause, Rui Werner Maçedo
Ultrasound-Triggered Release of 5-Fluorouracil from Soy Lecithin Echogenic Liposomes
title Ultrasound-Triggered Release of 5-Fluorouracil from Soy Lecithin Echogenic Liposomes
title_full Ultrasound-Triggered Release of 5-Fluorouracil from Soy Lecithin Echogenic Liposomes
title_fullStr Ultrasound-Triggered Release of 5-Fluorouracil from Soy Lecithin Echogenic Liposomes
title_full_unstemmed Ultrasound-Triggered Release of 5-Fluorouracil from Soy Lecithin Echogenic Liposomes
title_short Ultrasound-Triggered Release of 5-Fluorouracil from Soy Lecithin Echogenic Liposomes
title_sort ultrasound-triggered release of 5-fluorouracil from soy lecithin echogenic liposomes
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8229429/
https://www.ncbi.nlm.nih.gov/pubmed/34205990
http://dx.doi.org/10.3390/pharmaceutics13060821
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