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 Toxicológica, Centro de Ciências Naturais e Exatas, Universidade Federal de Santa Maria, RS, Brazil.
Eur J Pharm Sci. 2018 Jan 1;111:133-141. doi: 10.1016/j.ejps.2017.09.050. Epub 2017 Sep 28.
This study aimed the development of nanocapsules (NCs) for oral indole-3-carbinol (I3C) administration and evaluation of antinociceptive potential of this compound in its two forms, free and nanoencapsulated, using acute pain models. NCs showed adequate physicochemical characteristics and protected the I3C against UVC radiation exposure. It was observed no chemical bond between I3C and polymer by FTIR. Besides, X-ray and DSC analysis suggested that I3C was molecularly dispersed in NCs. The dialysis bag technique showed that almost 100% of the compound was released from NCs at 360min. Mathematical modeling demonstrated that this release occurred in two rates, with an initial burst effect followed by a slower release of I3C. Regarding the in vivo analysis, time-response curve showed that both forms of I3C caused an inhibition in inflammatory phase of nociception induced by formalin and increased the latency response in hot plate test. Interestingly, NCs were able to prolong the I3C effect in both tests. Furthermore, in dose-response curve, only I3C in its nanoencapsulated form presented effect on inflammatory phase of the formalin test. In conclusion, NCs to I3C incorporation presented adequate nanometric characteristics and prolonged its antinociceptive action in acute pain models tested.
本研究旨在开发用于吲哚-3-甲醇(I3C)口服给药的纳米胶囊(NCs),并评估游离和纳米包封两种形式的该化合物在急性疼痛模型中的镇痛潜力。NCs 表现出适当的物理化学特性,并能保护 I3C 免受 UVC 辐射暴露。FTIR 表明 I3C 和聚合物之间没有化学键。此外,X 射线和 DSC 分析表明 I3C 在 NCs 中呈分子分散状态。透析袋技术表明,NCs 在 360 分钟内几乎 100%释放了化合物。数学模型表明,这种释放以两种速率发生,初始突释效应后 I3C 以较慢的速率释放。关于体内分析,时间-反应曲线表明,两种形式的 I3C 均能抑制甲醛诱导的疼痛感受的炎症期,并增加热板试验中的潜伏期反应。有趣的是,NCs 能够延长两种测试中 I3C 的作用。此外,在剂量-反应曲线中,只有纳米包封形式的 I3C 对甲醛测试的炎症期有作用。总之,I3C 的 NCs 具有适当的纳米尺寸特性,并能延长其在急性疼痛模型中的镇痛作用。