Chassot Janaíne Micheli, Ribas Daniele, Silveira Elita Ferreira, Grünspan Lauren Dockhorn, Pires Camila Cervi, Farago Paulo Vitor, Braganhol Elizandra, Tasso Leandro, Cruz Letícia
J Nanosci Nanotechnol. 2015 Jan;15(1):855-64. doi: 10.1166/jnn.2015.9178.
The aim of this work was to develop polymeric nanocapsules intended for the pulmonary delivery of beclomethasone dipropionate using ethyl cellulose or poly(ε-caprolactone). The formulations showed adequate physicochemical characteristics, namely, average diameter lower than 260 nm, low polydispersity index (< 0.2), negative zeta potential, neutral pH values, and encapsulation efficiencies close to 100%. The thermal analysis by DSC suggested that beclomethasone dipropionate encapsulated in the nanocapsules was in an amorphous state. In addition, both ethyl cellulose and poly(ε-caprolactone) nanocapsules were able to delay the drug photodegradation under UVC radiation. The in vitro drug release showed a prolonged release without burst effect using the dialysis bag diffusion technique. Moreover, ethyl cellulose and poly(ε-caprolactone) nanocapsules presented low in vitro cytotoxicity on 3T3 fibroblasts cells. In vivo, the formulations showed no acute pulmonary injury in rats. Therefore, the developed nanocapsules could be considered suitable carriers to be used for beclomethasone dipropionate pulmonary delivery.
这项工作的目的是使用乙基纤维素或聚(ε-己内酯)开发用于丙酸倍氯米松肺部递送的聚合物纳米胶囊。这些制剂表现出足够的物理化学特性,即平均直径低于260nm,低多分散指数(<0.2),负ζ电位,中性pH值,以及接近100%的包封效率。DSC热分析表明,包裹在纳米胶囊中的丙酸倍氯米松处于无定形状态。此外,乙基纤维素和聚(ε-己内酯)纳米胶囊都能够在UVC辐射下延迟药物的光降解。使用透析袋扩散技术进行的体外药物释放显示出延长释放且无突释效应。此外,乙基纤维素和聚(ε-己内酯)纳米胶囊对3T3成纤维细胞表现出低体外细胞毒性。在体内,这些制剂在大鼠中未显示出急性肺损伤。因此,所开发的纳米胶囊可被认为是用于丙酸倍氯米松肺部递送的合适载体。