Bouchemal K, Briançon S, Perrier E, Fessi H, Bonnet I, Zydowicz N
Laboratoire d'Automatique et de Génie des Procédés, UMR-CNRS 5007 CPE Lyon, Université Claude Bernard Lyon 1, 43 Boulevard du 11 Novembre 1918, F-69622 Villeurbanne Cedex, France.
Int J Pharm. 2004 Jan 9;269(1):89-100. doi: 10.1016/j.ijpharm.2003.09.025.
Polyurethane polymers and poly(ether urethane) copolymers were chosen as drug carriers for alpha-tocopherol. This active ingredient is widely used as a strong antioxidant in many medical and cosmetic applications, but is rapidly degraded, because of its light, heat and oxygen sensitivity. Polyurethane and poly(ether urethane)-based nanocapsules were synthesized by interfacial reaction between two monomers. Interfacial polycondensation combined with spontaneous emulsification is a new technique for nanoparticles formation. Nanocapsules were characterized by studying particle size (150-500 nm), pH, yield of encapsulation and morphologies. Polyurethanes (PUR) were obtained from the condensation of diisocyanate (isophorone diisocyanate: IPDI) and polyol: 1,2-ethanediol (EG), 1,4-butanediol (BD), 1,6-hexanediol (HD). Poly(ether urethane) copolymers were obtained by replacing diols by polyethylene glycol oligomers (PEG) M(w) 200, 300, 400 and 600. Molecular weights of di- and polyols have a considerable influence on nanocapsules characteristics cited above. The increase of molecular weight of polyols tends to increase the mean size of nanocapsules from (232+/-3)nm using EG to (615+/-39)nm using PEG 600, and led to the apparition of a population of agglomerate particles. We also noted that the yield of encapsulation increases with the increase of polyol length (from 85.6 to 92.2% w/w). Microscopic observations confirmed particle size analysis, but cannot predict the membrane structure owing the small size of the particles.
聚氨酯聚合物和聚(醚 - 聚氨酯)共聚物被选作α - 生育酚的药物载体。这种活性成分在许多医学和化妆品应用中被广泛用作强抗氧化剂,但由于其对光、热和氧气敏感,会迅速降解。基于聚氨酯和聚(醚 - 聚氨酯)的纳米胶囊通过两种单体之间的界面反应合成。界面缩聚与自发乳化相结合是一种形成纳米颗粒的新技术。通过研究粒径(150 - 500纳米)、pH值、包封率和形态对纳米胶囊进行了表征。聚氨酯(PUR)由二异氰酸酯(异佛尔酮二异氰酸酯:IPDI)和多元醇:1,2 - 乙二醇(EG)、1,4 - 丁二醇(BD)、1,6 - 己二醇(HD)缩合得到。聚(醚 - 聚氨酯)共聚物通过用分子量为200、300、400和600的聚乙二醇低聚物(PEG)取代二醇来获得。二元醇和多元醇的分子量对上述纳米胶囊特性有相当大的影响。多元醇分子量的增加往往会使纳米胶囊的平均尺寸从使用EG时的(232±3)纳米增加到使用PEG 600时的(615±39)纳米,并导致出现团聚颗粒群体。我们还注意到包封率随着多元醇长度的增加而增加(从85.6%重量/重量增加到92.2%重量/重量)。显微镜观察证实了粒径分析,但由于颗粒尺寸小,无法预测膜结构。