首页> 外国专利> C6-C18 acylated hyaluronic acid derivative, method of preparation thereof, on the basis of nanomicellar composition, method of preparation thereof, and method of preparation of a stabilized nanomicellar composition and use thereof

C6-C18 acylated hyaluronic acid derivative, method of preparation thereof, on the basis of nanomicellar composition, method of preparation thereof, and method of preparation of a stabilized nanomicellar composition and use thereof

机译:C6-C18酰化透明质酸衍生物,基于纳米胶束组合物的制备方法,其制备方法,和稳定的纳米胶束组合物的制备方法及其用途

摘要

The invention relates to a method of preparation hydrophobized hyaluronic acid (Formula I) and further to a method of encapsulating biologically active substances into the nanomicelles of hydrophobized hyaluronan serving as carriers of biologically active hydrophobic substances. The hydrophobization of hyaluronan is carried out through an esterification reaction of hyaluronan with long-chain carboxylic acids, the latter being activated by a halogenide derivative of 2,4,6-trichlorobenzoic acid or by another organic chloride. In an aqueous environment, water-soluble hydrophobized derivatives can form nanomicelles in which nonpolar substances can be bound by means of non-covalent physical interactions. The core of a nanomicelle is formed by hydrophobic acyl functional groups while the shell of a nanomicelle is formed by hyaluronic acid. The encapsulation of the substances into nanomicelles can be performed by means of the solvent exchange method or by means of sonication. Hyaluronic nanomicelles support the penetration of bound substances in topical applications and enable the bound substances to be transferred into the individual cells. The nanomicelles obtained from hydrophobized hyaluronan derivatives are usable in cosmetic and pharmaceutical applications.
机译:本发明涉及一种制备疏水化的透明质酸的方法(式I),并且还涉及一种将生物活性物质包封到作为生物活性疏水性物质载体的疏水化透明质酸的纳米胶束中的方法。透明质酸的疏水化是通过透明质酸与长链羧酸的酯化反应进行的,长链羧酸被2,4,6-三氯苯甲酸的卤化物衍生物或另一种有机氯化物活化。在水性环境中,水溶性疏水化衍生物可形成纳米胶束,其中非极性物质可通过非共价物理相互作用键合。纳米胶束的核心由疏水性酰基官能团形成,而纳米胶束的壳由透明质酸形成。可以通过溶剂交换方法或通过超声处理将物质封装到纳米胶束中。透明质酸纳米胶束支持结合物质在局部应用中的渗透,并使结合物质能够转移到各个细胞中。从疏水化的透明质酸衍生物获得的纳米胶束可用于化妆品和药物应用中。

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