Anti-angiogenic activity of polymeric nanoparticles loaded with ursolic acid.

Abstract

Ursolic acid (UA) is an abundant natural product and has shown great promise for treating diseases related to the appearance of new blood vessels. However, its clinical use is limited due to its low solubility in aqueous media, resulting in reduced bioavailability. The present study aimed to synthetize poly(lactic-co-glycolic acid) nanoparticles loaded with UA by nanoprecipitation method and to evaluate the toxicity and anti-angiogenic activity using the in vivo chorioallantoic model. The nanoparticles were obtained in the size range that varied from 103.0 to 169.3 nm, they presented a uniform distribution (polydispersity index <0.2), and a negatively charged surface, with an encapsulation efficiency close to 50%. The release profile of the developed nanoformulation showed an initial burst in the first 2 h and demonstrated no acute toxicity (irritation index <0.9). Moreover, the chorioallantoic assay showed a significant reduction in both geometrical and topological parameters compared to saline control (p < .05). In conclusion, the study revealed a quick and simple way to obtain poly(lactic-co-glycolic) acid nanoparticles, a drug delivery system to UA, which showed potential antiangiogenic action and can be used to treat diseases involving neovascularisation.