Programa de Pós-graduação em Ciências Farmacêuticas, Centro de Ciências da Saúde, Universidade Federal de Santa Maria, Santa Maria, RS, Brazil.
Programa de Pós-Graduação em Bioquímica e Bioprospecção, Centro de Ciências Químicas, Farmacêuticas e de Alimentos, Universidade Federal de Pelotas, Pelotas, RS, Brazil.
Colloids Surf B Biointerfaces. 2015 Jun 1;130:272-7. doi: 10.1016/j.colsurfb.2015.04.023. Epub 2015 Apr 18.
This study aimed to prepare pomegranate seed oil nanoemulsions containing ketoprofen using pullulan as a polymeric stabilizer, and to evaluate antitumor activity against in vitro glioma cells. Formulations were prepared by the spontaneous emulsification method and different concentrations of pullulan were tested. Nanoemulsions presented adequate droplet size, polydispersity index, zeta potential, pH, ketoprofen content and encapsulation efficiency. Nanoemulsions were able to delay the photodegradation profile of ketoprofen under UVC radiation, regardless of the concentration of pullulan. In vitro release study indicates that nanoemulsions were able to release approximately 95.0% of ketoprofen in 5h. Free ketoprofen and formulations were considered hemocompatible at 1 μg/mL, in a hemolysis study, for intravenous administration. In addition, a formulation containing the highest concentration of pullulan was tested against C6 cell line and demonstrated significant activity, and did not reduce fibroblasts viability. Thus, pullulan can be considered an interesting excipient to prepare nanostructured systems and nanoemulsion formulations can be considered promising alternatives for the treatment of glioma.
本研究旨在制备含有酮洛芬的石榴籽油纳米乳，使用普鲁兰作为聚合物稳定剂，并评价其体外抗神经胶质瘤细胞的活性。通过自发乳化法制备制剂，并测试了不同浓度的普鲁兰。纳米乳具有合适的粒径、多分散指数、Zeta 电位、pH 值、酮洛芬含量和包封效率。纳米乳能够延迟 UVC 辐射下酮洛芬的光降解谱，而与普鲁兰的浓度无关。体外释放研究表明，纳米乳在 5 小时内能够释放约 95.0%的酮洛芬。在静脉给药的溶血研究中，游离酮洛芬和制剂在 1μg/mL 时被认为具有良好的血液相容性。此外，还对含有最高浓度普鲁兰的制剂进行了 C6 细胞系的测试，结果表明其具有显著的活性，且不会降低成纤维细胞的活力。因此，普鲁兰可以被认为是一种制备纳米结构系统的有趣赋形剂，纳米乳制剂可以被认为是治疗神经胶质瘤的有前途的替代方案。
