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蛋白质、多糖及其复合物作为乳化剂稳定剂:在制药领域替代合成表面活性剂的选择?

Proteins, polysaccharides, and their complexes used as stabilizers for emulsions: alternatives to synthetic surfactants in the pharmaceutical field?

机构信息

Univ Paris Sud, Faculté de Pharmacie, 5 rue Jean-Baptiste Clément, 92296, Châtenay-Malabry Cedex, France.

出版信息

Int J Pharm. 2012 Oct 15;436(1-2):359-78. doi: 10.1016/j.ijpharm.2012.06.052. Epub 2012 Jul 1.

Abstract

Emulsions are widely used in pharmaceutics for the encapsulation, solubilization, entrapment, and controlled delivery of active ingredients. In order to answer the increasing demand for clean label excipients, natural polymers can replace the potentially irritative synthetic surfactants used in emulsion formulation. Indeed, biopolymers are currently used in the food industry to stabilize emulsions, and they appear as promising candidates in the pharmaceutical field too. All proteins and some polysaccharides are able to adsorb at a globule surface, thus decreasing the interfacial tension and enhancing the interfacial elasticity. However, most polysaccharides stabilize emulsions simply by increasing the viscosity of the continuous phase. Proteins and polysaccharides may also be associated either through covalent bonding or electrostatic interactions. The combination of the properties of these biopolymers under appropriate conditions leads to increased emulsion stability. Alternative layers of oppositely charged biopolymers can also be formed around the globules to obtain multi-layered "membranes". These layers can provide electrostatic and steric stabilization thus improving thermal stability and resistance to external treatment. The novel biopolymer-stabilized emulsions have a great potential in the pharmaceutical field for encapsulation, controlled digestion, and targeted release although several challenging issues such as storage and bacteriological concerns still need to be addressed.

摘要

乳液在药剂学中被广泛用于封装、溶解、包埋和控制活性成分的释放。为了满足对清洁标签赋形剂日益增长的需求,天然聚合物可以替代乳液配方中可能具有刺激性的合成表面活性剂。事实上,生物聚合物目前被用于食品工业来稳定乳液,它们在制药领域也显示出了良好的应用前景。所有蛋白质和一些多糖都能够在液滴表面吸附,从而降低界面张力并增强界面弹性。然而,大多数多糖通过增加连续相的粘度来简单地稳定乳液。蛋白质和多糖也可以通过共价键或静电相互作用结合在一起。在适当的条件下,这些生物聚合物的特性相结合会导致乳液稳定性增加。相反电荷的生物聚合物的替代层也可以在液滴周围形成,以获得多层“膜”。这些层可以提供静电和空间稳定作用,从而提高热稳定性和对外部处理的抵抗力。新型生物聚合物稳定的乳液在制药领域具有很大的潜力,可用于封装、控制消化和靶向释放,尽管仍然需要解决一些具有挑战性的问题,如储存和细菌学问题。

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