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Evaluation of Antitumor Activity of Long-Circulating and pH-Sensitive Liposomes Containing Ursolic Acid in Animal Models of Breast Tumor and Gliosarcoma. | LitMetric

AI Article Synopsis

  • Ursolic acid (UA) is a plant-derived triterpene known for its antitumor properties, but its low water solubility limits its effectiveness, prompting the development of a new delivery system using long-circulating and pH-sensitive liposomes (SpHL-UA).
  • In experiments with murine brain cancer and human breast tumor models, researchers assessed the antiangiogenic effects of free UA and SpHL-UA treatments through various methods, including tumor volume measurement and imaging techniques.
  • The results indicated that while there was minimal tumor growth inhibition in murine gliosarcoma, SpHL-UA suggested potential antiangiogenic effects in the human breast tumor model, although overall effects were not statistically significant.

Article Abstract

Background Ursolic acid (UA) is a triterpene found in different plant species, possessing antitumor activity, which may be a result of its antiangiogenic effect. However, UA has low water solubility, which limits its use because the bioavailability is impaired. To overcome this inconvenience, we developed long-circulating and pH-sensitive liposomes containing ursolic acid (SpHL-UA). We investigated the antiangiogenic effect of free UA and SpHL-UA in murine brain cancer and human breast tumor models by means of determination of the relative tumor volume, dynamic contrast-enhanced magnetic resonance imaging (DCE-MRI), and histopathological analysis. Methods The animals were treated with dimethyl sulfoxide in 0.9% (w/v) NaCl, free UA, long-circulating and pH-sensitive liposomes without drug (SpHL), or SpHL-UA. The animals were submitted to each treatment by intraperitoneal injection for 5 days. The dose of free UA or SpHL-UA was equal to 23 mg/kg. Results Tumor growth inhibition was not observed in human breast tumor-bearing animals. For murine gliosarcoma-bearing animals, a slight tumor growth inhibition was observed in the groups treated with free UA or SpHL-UA (9% and 15%, respectively). No significant change in any of the parameters evaluated by DCE-MRI for both experimental models could be observed. Nevertheless, the evaluation of the mean values of magnetic resonance parameters of human breast tumor-bearing animals showed evidence of a possible antiangiogenic effect induced by SpHL-UA. Histopathological analysis did not present significant change for any treatment. Conclusion SpHL-UA did not show antiangiogenic activity in a gliosarcoma model and seemed to induce an antiangiogenic effect in the human breast tumor model.

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Source
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5739155PMC
http://dx.doi.org/10.1177/1534735416628273DOI Listing

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