Ribeiro Ana F, Santos Juliana F, Mattos Rômulo R, Barros Eliane G O, Nasciutti Luiz Eurico, Cabral Lúcio M, Sousa Valeria P DE
Departamento de Fármacos e Medicamentos, Faculdade de Farmácia, Universidade Federal do Rio de Janeiro, Av. Carlos Chagas Filho, 373, CCS, 21941-902 Rio de Janeiro, RJ, Brazil.
Faculdade de Farmácia, Federal Institute of Education, Science and Technology of Rio de Janeiro, Rua Professor Carlos Wenceslau, 343, 21715-000 Rio de Janeiro, RJ, Brazil.
An Acad Bras Cienc. 2020 Apr 17;92(1):e20190336. doi: 10.1590/0001-3765202020190336. eCollection 2020.
Uncaria tomentosa (UT) extracts have been shown to have promising anti-tumor activity. We hypothesized that its incorporation into nanostructured systems could improve the anticancer properties. Here, poly-e-caprolactone (PCL) and poly-d,l-lactide-co-glycolide (PLGA) were employed to generate nanoparticles loaded with UT extract in a single emulsion solvent evaporation method. The nanoparticles were characterized by particle size, zeta potential, morphology and entrapment efficiency along with stability and release profiles. The nanoparticles presented entrapment efficiencies above 60% and a mean diameter below 300nm. UT-PCL nanoparticles presented higher entrapment efficiency and mean particle size as well as a slow release rate. The UT-PLGA nanoparticles showed higher drug loading. Two prostate cancer cell-lines, LNCaP and DU145 that were derived from metastatic sites, served as model systems to assess cytotoxicity and anti-cancer activity. In vitro, both formulations reduced the viability of DU145 and LNCaP cells. Yet, the UT-PLGA nanoparticles showed higher cytotoxicity towards DU145 cells while the UTPCL against LNCaP cells. The results confirm that the incorporation of UT into nanoparticles could enhance its anti-cancer activities that can offer a viable alternative for the treatment of prostrate canner and highlights the potential of nanostructured systems to provide a promising methodology to enhance the activity of natural extracts.
毛钩藤提取物已显示出有前景的抗肿瘤活性。我们推测将其纳入纳米结构系统可改善其抗癌特性。在此，采用聚己内酯（PCL）和聚（d，l-丙交酯-共-乙交酯）（PLGA）通过单乳液溶剂蒸发法制备负载毛钩藤提取物的纳米颗粒。通过粒径、zeta电位、形态、包封率以及稳定性和释放曲线对纳米颗粒进行表征。纳米颗粒的包封率高于60%，平均直径低于300nm。毛钩藤-PCL纳米颗粒具有更高的包封率和平均粒径以及较慢的释放速率。毛钩藤-PLGA纳米颗粒显示出更高的载药量。两种源自转移部位的前列腺癌细胞系LNCaP和DU145用作评估细胞毒性和抗癌活性的模型系统。在体外，两种制剂均降低了DU145和LNCaP细胞的活力。然而，毛钩藤-PLGA纳米颗粒对DU145细胞显示出更高的细胞毒性，而毛钩藤-PCL纳米颗粒对LNCaP细胞的细胞毒性更高。结果证实将毛钩藤纳入纳米颗粒可增强其抗癌活性，这可为前列腺癌的治疗提供一种可行的替代方案，并突出了纳米结构系统提供一种有前景的方法来增强天然提取物活性的潜力。
