The role of size in PEGylated liposomal doxorubicin biodistribution and anti‐tumour activity
Abstract The size of nanoliposome‐encapsulated drugs significantly affects their therapeutic efficacy, biodistribution, targeting ability, and toxicity profile for the cancer treatment. In the present study, the biodistribution and anti‐tumoral activity of PEGylated liposomal Doxorubicin (PLD) formu...
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2022-09-01
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Online Access: | https://doi.org/10.1049/nbt2.12094 |
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author | Saba Dadpour Amin Mehrabian Mahdieh Arabsalmani Elaheh Mirhadi Anis Askarizadeh Mohammad Mashreghi Mahmoud Reza Jaafari |
author_facet | Saba Dadpour Amin Mehrabian Mahdieh Arabsalmani Elaheh Mirhadi Anis Askarizadeh Mohammad Mashreghi Mahmoud Reza Jaafari |
author_sort | Saba Dadpour |
collection | DOAJ |
description | Abstract The size of nanoliposome‐encapsulated drugs significantly affects their therapeutic efficacy, biodistribution, targeting ability, and toxicity profile for the cancer treatment. In the present study, the biodistribution and anti‐tumoral activity of PEGylated liposomal Doxorubicin (PLD) formulations with different sizes were investigated. First, 100, 200, and 400 nm PLDs were prepared by remote loading procedure and characterised for their size, zeta potential, encapsulation efficacy, and release properties. Then, in vitro cellular uptake and cytotoxicity were studied by flow cytometry and MTT assay, and compared with commercially available PLD Caelyx®. In vivo studies were applied on BALB/c mice bearing C26 colon carcinoma. The cytotoxicity and cellular uptake tests did not demonstrate any statistically significant differences between PLDs. The biodistribution results showed that Caelyx® and 100 nm liposomal formulations had the most doxorubicin (Dox) accumulation in the tumour tissue and, as a result, considerably suppressed tumour growth compared with 200 and 400 nm PLDs. In contrast, larger nanoparticles (200 and 400 nm formulations) had more accumulation in the liver and spleen. This study revealed that 90 nm Caelyx® biodistribution profile led to the stronger anti‐tumour activity of the drug and hence significant survival extension, and showed the importance of vesicle size in the targeting of nanoparticles to the tumour microenvironment for the treatment of cancer. |
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id | doaj-art-976762e36fb642269d4acca83f69b3d4 |
institution | Kabale University |
issn | 1751-8741 1751-875X |
language | English |
publishDate | 2022-09-01 |
publisher | Wiley |
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series | IET Nanobiotechnology |
spelling | doaj-art-976762e36fb642269d4acca83f69b3d42025-02-03T06:47:36ZengWileyIET Nanobiotechnology1751-87411751-875X2022-09-01167-825927210.1049/nbt2.12094The role of size in PEGylated liposomal doxorubicin biodistribution and anti‐tumour activitySaba Dadpour0Amin Mehrabian1Mahdieh Arabsalmani2Elaheh Mirhadi3Anis Askarizadeh4Mohammad Mashreghi5Mahmoud Reza Jaafari6Nanotechnology Research Center Student Research Committee Faculty of Pharmacy Mashhad University of Medical Sciences Mashhad IranNanotechnology Research Center Pharmaceutical Technology Institute Mashhad University of Medical Sciences Mashhad IranNanotechnology Research Center Pharmaceutical Technology Institute Mashhad University of Medical Sciences Mashhad IranNanotechnology Research Center Pharmaceutical Technology Institute Mashhad University of Medical Sciences Mashhad IranNanotechnology Research Center Pharmaceutical Technology Institute Mashhad University of Medical Sciences Mashhad IranNanotechnology Research Center Pharmaceutical Technology Institute Mashhad University of Medical Sciences Mashhad IranNanotechnology Research Center Pharmaceutical Technology Institute Mashhad University of Medical Sciences Mashhad IranAbstract The size of nanoliposome‐encapsulated drugs significantly affects their therapeutic efficacy, biodistribution, targeting ability, and toxicity profile for the cancer treatment. In the present study, the biodistribution and anti‐tumoral activity of PEGylated liposomal Doxorubicin (PLD) formulations with different sizes were investigated. First, 100, 200, and 400 nm PLDs were prepared by remote loading procedure and characterised for their size, zeta potential, encapsulation efficacy, and release properties. Then, in vitro cellular uptake and cytotoxicity were studied by flow cytometry and MTT assay, and compared with commercially available PLD Caelyx®. In vivo studies were applied on BALB/c mice bearing C26 colon carcinoma. The cytotoxicity and cellular uptake tests did not demonstrate any statistically significant differences between PLDs. The biodistribution results showed that Caelyx® and 100 nm liposomal formulations had the most doxorubicin (Dox) accumulation in the tumour tissue and, as a result, considerably suppressed tumour growth compared with 200 and 400 nm PLDs. In contrast, larger nanoparticles (200 and 400 nm formulations) had more accumulation in the liver and spleen. This study revealed that 90 nm Caelyx® biodistribution profile led to the stronger anti‐tumour activity of the drug and hence significant survival extension, and showed the importance of vesicle size in the targeting of nanoparticles to the tumour microenvironment for the treatment of cancer.https://doi.org/10.1049/nbt2.12094BiodistributionCancerEPR effectNanoparticle sizePEGylated liposomal doxorubicinTherapeutic efficacy |
spellingShingle | Saba Dadpour Amin Mehrabian Mahdieh Arabsalmani Elaheh Mirhadi Anis Askarizadeh Mohammad Mashreghi Mahmoud Reza Jaafari The role of size in PEGylated liposomal doxorubicin biodistribution and anti‐tumour activity IET Nanobiotechnology Biodistribution Cancer EPR effect Nanoparticle size PEGylated liposomal doxorubicin Therapeutic efficacy |
title | The role of size in PEGylated liposomal doxorubicin biodistribution and anti‐tumour activity |
title_full | The role of size in PEGylated liposomal doxorubicin biodistribution and anti‐tumour activity |
title_fullStr | The role of size in PEGylated liposomal doxorubicin biodistribution and anti‐tumour activity |
title_full_unstemmed | The role of size in PEGylated liposomal doxorubicin biodistribution and anti‐tumour activity |
title_short | The role of size in PEGylated liposomal doxorubicin biodistribution and anti‐tumour activity |
title_sort | role of size in pegylated liposomal doxorubicin biodistribution and anti tumour activity |
topic | Biodistribution Cancer EPR effect Nanoparticle size PEGylated liposomal doxorubicin Therapeutic efficacy |
url | https://doi.org/10.1049/nbt2.12094 |
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