da Fonseca Letícia Sias, Silveira Rodrigo Paulo, Deboni Alberto Marçal, Benvenutti Edilson Valmir, Costa Tânia M H, Guterres Sílvia S, Pohlmann Adriana R
Programa de Pós-Graduação em Química, Instituto de Química, Universidade Federal do Rio Grande do Sul, CP 15003, Porto Alegre, RS, Brazil.
Int J Pharm. 2008 Jun 24;358(1-2):292-5. doi: 10.1016/j.ijpharm.2008.02.005. Epub 2008 Feb 15.
The aim of this work was to evaluate the potentiality to control the drug release of a new architecture of microparticles organized at the nanoscopic scale by assembling polymeric nanocapsules at the surface of drug-loaded xerogels. Xerogel was prepared by sol-gel method using sodium diclofenac, as hydrophilic drug model, and coated by spray-drying. After coating, the surface areas decreased from 82 to 28 m(2)/g, the encapsulation efficiency was 71% and SEM analysis showed irregular microparticles coated by the nanocapsules. Formulation showed satisfactory gastro-resistance presenting drug release lower than 3% (60 min) in acid medium. In water, the pure drug dissolved 92% after 5 min, uncoated drug-loaded xerogel released 60% and nanocapsule coated drug-loaded xerogel 36%. After 60 min, uncoated drug-loaded xerogel released 82% and nanocapsule coated drug-loaded xerogel 62%. In conclusion, the new system was able to control the release of the hydrophilic drug model.
这项工作的目的是评估通过在载药干凝胶表面组装聚合物纳米胶囊来控制纳米级组织的新型微粒结构药物释放的潜力。使用双氯芬酸钠作为亲水性药物模型,通过溶胶 - 凝胶法制备干凝胶,并通过喷雾干燥进行包衣。包衣后,表面积从82降至28 m²/g,包封效率为71%,扫描电子显微镜分析显示纳米胶囊包衣的微粒不规则。制剂表现出令人满意的胃抗性,在酸性介质中药物释放低于3%(60分钟)。在水中,纯药物在5分钟后溶解92%,未包衣的载药干凝胶释放60%,纳米胶囊包衣的载药干凝胶释放36%。60分钟后,未包衣的载药干凝胶释放82%,纳米胶囊包衣的载药干凝胶释放62%。总之,新系统能够控制亲水性药物模型的释放。