Hamoudi M, Trichard L, Grossiord J-L, Chaminade P, Duchêne D, Le Bas G, Fattal E, Bochot A
CNRS UMR 8612, physicochimie-pharmacotechnie-biopharmacie, faculté de pharmacie, université Paris-Sud, 5, rue Jean-Baptiste-Clément, 92296 Châtenay-Malabry, France.
Ann Pharm Fr. 2009 Nov;67(6):391-8. doi: 10.1016/j.pharma.2009.08.003. Epub 2009 Oct 14.
Natural cyclodextrins are cyclic oligosaccharides which can be modified to obtain more water soluble or insoluble derivatives. The main interest of cyclodextrins results from their ability to form an inclusion complex with hydrophobic molecules. Inclusion constitutes a true molecular encapsulation. This property is employed in pharmaceutical industry to facilitate the formulation of poorly water soluble and/or fragile drugs. A more recent application of cyclodextrins consists in their use in the preparation of dispersed systems such as micro- and nanoparticles or even liposomes. When incorporated in dispersed systems, cyclodextrin can enhance drug solubility, drug stability and drug loading. Interestingly, cyclodextrins themselves can also be employed to form or stabilise dispersed systems (material or emulsifying agent). For example, the interactions between cyclodextrins with components of the vegetable oils (more especially with triglycerides) allow to stabilise simple or multiple emulsions but also to form particles called "beads". Very rich in oil, this novel lipid carrier presents an important potential for the encapsulation of highly lipophilic compounds and their delivery by topical and oral routes. These two applications are more particularly developed in the present paper.
天然环糊精是环状寡糖，可以进行修饰以获得更易溶于水或不溶于水的衍生物。环糊精的主要价值在于它们能够与疏水分子形成包合物。包合构成了一种真正的分子封装。这一特性在制药工业中被用于促进难溶性和/或易分解药物的制剂制备。环糊精的一个较新应用是用于制备分散体系，如微纳米颗粒甚至脂质体。当环糊精掺入分散体系中时，它可以提高药物溶解度、药物稳定性和载药量。有趣的是，环糊精本身也可用于形成或稳定分散体系（材料或乳化剂）。例如，环糊精与植物油成分（尤其是甘油三酯）之间的相互作用能够稳定单乳液或多重乳液，还能形成所谓的“珠粒”颗粒。这种富含油脂的新型脂质载体在封装高亲脂性化合物以及通过局部和口服途径递送这些化合物方面具有重要潜力。本文将更详细地阐述这两种应用。
