Weber Julia, Funk Nadine L, Motta Mariana H, Guedes Alessandra M, Visintainer Ana Paula C, Tedesco Solange B, Da Silva Cristiane de B
J Nanosci Nanotechnol. 2016 Feb;16(2):1354-62. doi: 10.1166/jnn.2016.11674.
The association of vegetable products to nanostructured systems has attracted the attention of researchers due to several advantages, such as drug photoprotection, as well as the improvement of the pharmacological and therapeutic activities because of synergistic action, which can provide their topical application. In this work, lipid-core nanocapsules containing borage oil as oil core and betamethasone dipropionate were developed, and nanocapsules without the drug were prepared for comparison. The suspensions were characterized in relation to mean particle size, zeta potential, pH, drug content, and encapsulation efficiency. A photodegradation study was carried out and the in vitro release profile as well as the irritation potential of the drug after nanoencapsulation were also evaluated. In addition, the antiproliferative activity of the free borage oil as well as loaded in nanocapsules was studied. Lipid-core nanocapsules showed nanometric mean size (185-210 nm); polydispersity index below 0.10; negative zeta potential and pH slightly acid (6.0-6.2). Moreover, the drug content was close to theoretical concentration (0.50 +/- 0.03 mg/ml of betamethasone), and the encapsulation efficiency was approximately 100%. The study of the antiproliferative activity of borage oil showed ability to reduce cell growth of Allium cepa. The nanoencapsulation of betamethasone dipropionate provided greater protection against UVC light and decreased the irritation potential of the drug. The release profile of betamethasone dipropionate from nanocapsules followed monoexponential model.
由于多种优势，如药物光保护以及协同作用带来的药理和治疗活性的提高，可实现其局部应用，植物产品与纳米结构系统的结合吸引了研究人员的关注。在这项工作中，制备了以琉璃苣油为油核、二丙酸倍他米松为药物的脂质核纳米胶囊，并制备了不含药物的纳米胶囊用于比较。对悬浮液的平均粒径、zeta电位、pH值、药物含量和包封率进行了表征。开展了光降解研究，并评估了纳米包封后药物的体外释放曲线以及刺激潜力。此外，还研究了游离琉璃苣油以及负载在纳米胶囊中的琉璃苣油的抗增殖活性。脂质核纳米胶囊显示出纳米级的平均尺寸（185 - 210 nm）；多分散指数低于0.10；zeta电位为负，pH值呈微酸性（6.0 - 6.2）。此外，药物含量接近理论浓度（二丙酸倍他米松为0.50 +/- 0.03 mg/ml），包封率约为100%。琉璃苣油抗增殖活性的研究表明其具有降低洋葱细胞生长的能力。二丙酸倍他米松的纳米包封提供了对UVC光的更大保护，并降低了药物的刺激潜力。二丙酸倍他米松从纳米胶囊中的释放曲线符合单指数模型。
