Sari Marcel Henrique Marcondes, Ferreira Luana Mota, AngonesiZborowski Vanessa, Araujo Paulo Cesar Oliveira, Nadal Jessica Mendes, Farago Paulo Vitor, Cruz Letícia, Nogueira Cristina Wayne
Programa de Pós-graduação em Bioquímica Toxicológica, Laboratório de Síntese, Reatividade e Avaliação Farmacológica e Toxicológica de Organocalcogênios. Departamento de Biologia Molecular, Centro de Ciências Naturais e Exatas, Universidade Federal de Santa Maria, Santa Maria, Zip code 97105-900, RS, Brazil.
Programa de Pós-graduação em Ciências Farmacêuticas, Laboratório de Tecnologia Farmacêutica. Departamento de Farmácia Industrial, Centro de Ciências da Saúde, Universidade Federal de Santa Maria, Santa Maria, Zip code 97105-900, RS, Brazil.
Colloids Surf B Biointerfaces. 2017 Sep 1;157:464-472. doi: 10.1016/j.colsurfb.2017.06.016. Epub 2017 Jun 20.
The p,p'-methoxyl-diphenyl diselenide [(OMePhSe)2] is an, organoselenium compound that elicits antinociceptive action in different, animal models of pain. However, the compound has physicochemical, Limitations that delay its clinical studies. Herein, (OMePhSe)2, nanocapsules were developed and their physicochemical properties were, analyzed using different techniques (Scanning electron microscopy with, field emissionguns, wide-angle X-ray diffractometry, fourier-transform, infrared spectroscopy, thermogravimetric analysis and differential, scanning calorimetry). The antinociceptive action of (OMePhSe)2 free or, nanoencapsulated was evaluated in an animal model of thermal nociception., The (OMePhSe)2 nanocapsules or the free compound (25mg/kg, 10ml/kg), were administered to Swiss mice by the intragastric (i.g.), intraperitoneal (i.p.) or subcutaneous (s.c.) route in a single or, repeated administration regimen. The (OMePhSe)2 nanocapsules had, spherical shape, no chemical interaction among the formulation components, and high thermal stability. Treatment with (OMePhSe)2 elicited an, antinociceptive action independent of the administration route and, regimen schedule. The (OMePhSe)2 incorporation into nanocapsules, prolonged and improved the compound antinociceptive action. The, (OMePhSe)2 antinociceptive action was influenced by the route of, administration (intragastric>intraperitoneal>subcutaneous) and by the, vehicle used (NCs>canola oil). Altogether, the current study, demonstrated that the (OMePhSe)2 nanoencapsulation increased the compound, thermal stability and the antinociceptive action in mice, suggesting that, the polymeric nanocapsules provided advantages in comparison to the free, compound form.
对,对'-甲氧基二苯基二硒醚[(OMePhSe)2]是一种有机硒化合物,在不同的疼痛动物模型中引发抗伤害感受作用。然而,该化合物具有物理化学局限性,这延迟了其临床研究。在此,开发了(OMePhSe)2纳米胶囊,并使用不同技术(场发射枪扫描电子显微镜、广角X射线衍射法、傅里叶变换红外光谱、热重分析和差示扫描量热法)分析了它们的物理化学性质。在热伤害感受动物模型中评估了游离或纳米包封的(OMePhSe)2的抗伤害感受作用。将(OMePhSe)2纳米胶囊或游离化合物(25mg/kg,10ml/kg)通过胃内(i.g.)、腹腔内(i.p.)或皮下(s.c.)途径以单次或重复给药方案给予瑞士小鼠。(OMePhSe)2纳米胶囊呈球形,制剂成分之间无化学相互作用,且具有高热稳定性。用(OMePhSe)2治疗引发了与给药途径和方案时间表无关的抗伤害感受作用。将(OMePhSe)2掺入纳米胶囊中延长并改善了该化合物的抗伤害感受作用。(OMePhSe)2的抗伤害感受作用受给药途径(胃内>腹腔内>皮下)和所用载体(纳米胶囊>菜籽油)的影响。总之,当前研究表明,(OMePhSe)2纳米包封提高了该化合物在小鼠中的热稳定性和抗伤害感受作用,表明与游离化合物形式相比,聚合物纳米胶囊具有优势。