Chausson Mickael, Fluchère Ann-Sophie, Landreau Emmanuel, Aguni Youssef, Chevalier Yves, Hamaide Thierry, Abdul-Malak Nabil, Bonnet Isabelle
Université de Lyon, Laboratoire d'Automatique et de Génie des Procédés, LAGEP, UMR CNRS 5007, Bât 308, 43 Bd 11 Novembre, 69622 Villeurbanne Cedex, France.
Int J Pharm. 2008 Oct 1;362(1-2):153-62. doi: 10.1016/j.ijpharm.2008.06.007. Epub 2008 Jun 14.
Block copolymers poly(caprolactone)-block-poly(ethylene oxide) are promising non-ionic macromolecular surfactants for the stabilization of emulsions because they display a stronger adsorption and provide an increased long-term stability. But such amphiphilic copolymers should also allow the fabrication of the suspensions according to the emulsification process used. An evaluation of such block copolymers was done regarding the nanoprecipitation and the miniemulsion polymerization processes that both afford aqueous suspensions of nanoparticles. Both the fabrication and the long-term stability were investigated. It was found that the emulsification by means of the nanoprecipitation process was successful when the amphiphilic block copolymer was added into the organic phase. The studies on the structure-activity relationships have shown that a minimum length of the poly(ethylene oxide) block was necessary in order to ensure both the long-term colloidal stability of the suspensions and the instantaneous stability during the preparation process. The length of the hydrophobic block was a parameter of less relevance, but a minimum length was required for the copolymers to be soluble in the organic phase. The miniemulsion polymerization process using block copolymer emulsifiers could be adapted to the incorporation of large loads of vitamin E acetate used as a hydrophobe stabilizer.
嵌段共聚物聚己内酯-嵌段-聚环氧乙烷是用于稳定乳液的有前途的非离子大分子表面活性剂,因为它们表现出更强的吸附作用并提供更高的长期稳定性。但这种两亲性共聚物还应根据所使用的乳化工艺来制备悬浮液。针对纳米沉淀法和微乳液聚合工艺对这类嵌段共聚物进行了评估,这两种方法都能得到纳米颗粒的水悬浮液。对制备过程和长期稳定性都进行了研究。结果发现,当将两亲性嵌段共聚物加入有机相时,通过纳米沉淀法进行乳化是成功的。结构-活性关系研究表明,聚环氧乙烷嵌段需要有最小长度,以确保悬浮液的长期胶体稳定性以及制备过程中的瞬时稳定性。疏水嵌段的长度是相关性较小的一个参数,但共聚物要可溶于有机相则需要有最小长度。使用嵌段共聚物乳化剂的微乳液聚合工艺可以适用于加入大量用作疏水稳定剂的维生素E醋酸酯。