ArticleCancer chemotherapy and pharmacology2026
Antitumor efficacy and reduced systemic toxicity of palmitic acid-modified pirarubicin nanoparticles in mice.
Article in Cancer chemotherapy and pharmacology, 2026. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.
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Abstract
purposePirarubicin (THP) is a potent anthracycline anticancer agent; however, its clinical use is limited by nonselective tissue distribution and systemic toxicity. This study aimed to evaluate whether palmitic acid-modified THP nanoparticles (Pal-THP nanoparticles) could improve the in vivo therapeutic profile of THP.
methodsPal-THP nanoparticles stabilized by albumin as a formulation stabilizer were prepared by antisolvent precipitation. Antitumor efficacy, biodistribution, and drug forms (intact Pal-THP and the free THP released from Pal-THP) were evaluated in colon 26 tumor-bearing mice following intravenous administration. Acute systemic and hemolytic toxicity were assessed relative to THP.
resultsPal-THP nanoparticles significantly suppressed tumor growth compared with the control group, without inducing body weight loss, whereas THP exhibited a tendency toward tumor suppression but did not reach statistical significance versus control at an equivalent dose. While the absolute tumor accumulation of Pal-THP nanoparticles was limited, it was significantly higher than that of THP. Importantly, there was efficient conversion of Pal-THP to free THP in tumor tissue, which is consistent with the presence of an acid‑labile hydrazone linkage. Pal-THP nanoparticles also markedly attenuated acute systemic and hemolytic toxicity, in contrast to THP, under the present experimental conditions.
conclusionPal-THP nanoparticles altered the in vivo fate of THP through tumor accumulation and tumor-localized conversion to free THP. This resulted in effective tumor suppression and a significant reduction in toxicity compared to THP in mice. Thus, this formulation strategy represents a promising approach for improving the therapeutic index of chemotherapy using THP and other anthracyclines.
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