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Polyamino acids functionalized by hydrophobic grafts bearing an anionic charge and applications thereof, such as therapeutic applications

机译:由带有阴离子电荷的疏水接枝官能化的聚氨基酸及其应用,例如治疗应用

摘要

The present invention relates to novel materials based on biodegradable polyamino acids that are useful especially for the vectorization of active principle(s) (AP). The invention further relates to novel pharmaceutical, cosmetic, dietetic or phytosanitary compositions based on these polyamino acids. The object of the invention is to provide a novel polymer starting material that is capable of being used for the vectorization of AP and makes it possible on the one hand to achieve high polymer/AP ratios, and on the other hand optimally to satisfy all the specifications required in the case in point: biocompatibility, biodegradability, ability to associate easily with numerous active principles or to solubilize them, and ability to release these active principles in vivo. This object is achieved by the present invention, which relates first and foremost to linear polyamino acids comprising aspartic units or glutamic units and having hydrophobic grafts comprising hydrophobic groups containing from 8 to 30 carbon atoms, at least one of these hydrophobic grafts having at least one anionic charge and/or one or more mutually identical or different ionizable groups each capable of giving rise to at least one anionic charge. These polymers are amphiphilic and anionic and are capable of being converted easily and economically to particles for the vectorization of active principles, these particles themselves being capable of forming stable aqueous colloidal suspensions.
机译:本发明涉及基于可生物降解的聚氨基酸的新型材料,其特别用于有效成分(AP)的矢量化。本发明进一步涉及基于这些聚氨基酸的新型药物,化妆品,饮食或植物检疫组合物。发明内容本发明的目的是提供一种新颖的聚合物起始材料,其能够用于AP的矢量化,并且一方面可以实现高的聚合物/ AP比,另一方面可以最佳地满足所有的要求。就此而言,所需的规范是:生物相容性,生物降解性,与众多活性成分容易结合或溶解的能力,以及在体内释放这些活性成分的能力。该目的通过本发明得以实现,本发明首先涉及包含天冬氨酸单元或谷氨酸单元并且具有包含8至30个碳原子的疏水基团的疏水接枝的线性聚氨基酸,这些疏水接枝中的至少一个具有至少一个。阴离子电荷和/或一个或多个彼此相同或不同的可电离基团,它们各自能够产生至少一个阴离子电荷。这些聚合物是两亲性和阴离子性的,能够容易且经济地转化为用于活性成分矢量化的颗粒,这些颗粒本身能够形成稳定的水性胶体悬浮液。

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