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In the present study, the biodistribution and anti\u2010tumoral activity of PEGylated liposomal Doxorubicin (PLD) formulations with different sizes were investigated. First, 100, 200, and 400\u00a0nm 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\n                    <jats:sup>\u00ae<\/jats:sup>\n                    . 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\n                    <jats:sup>\u00ae<\/jats:sup>\n                    and 100\u00a0nm 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\u00a0nm PLDs. In contrast, larger nanoparticles (200 and 400\u00a0nm formulations) had more accumulation in the liver and spleen. This study revealed that 90\u00a0nm Caelyx\n                    <jats:sup>\u00ae<\/jats:sup>\n                    biodistribution profile led to the stronger anti\u2010tumour 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.\n                  <\/jats:p>","DOI":"10.1049\/nbt2.12094","type":"journal-article","created":{"date-parts":[[2022,8,19]],"date-time":"2022-08-19T01:54:44Z","timestamp":1660874084000},"page":"259-272","update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":35,"title":["The role of size in PEGylated liposomal doxorubicin biodistribution and anti\u2010tumour 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