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首页> 外国专利> C6-C18-acylated hyaluronate-based nanomicellar composition, process for preparing C6-C18-acylated hyaluronate, process for preparing nanomicellar composition and stabilized nanomicellar composition as well as use thereof

C6-C18-acylated hyaluronate-based nanomicellar composition, process for preparing C6-C18-acylated hyaluronate, process for preparing nanomicellar composition and stabilized nanomicellar composition as well as use thereof

机译：C6-C18-酰化透明质酸盐基纳米胶束组合物，制备C6-C18-酰化透明质酸盐的方法，制备纳米胶束组合物和稳定的纳米胶束组合物及其用途

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摘要

The present invention relates to a process for preparing hydrophobized hyaluronate (of the general formula I) and further to a method of encapsulating biologically active substances into the nanomicelles of the hydrophobized hyaluronate serving as a carrier of biologically active hydrophobic substances. The hydrophobization of hyaluronate is carried out through an esterification reaction of hyaluronate with long-chain carboxylic acids, the latter being activated by a halide 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 hyaluronate. 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 hyaluronate derivatives are usable in cosmetic and pharmaceutical applications.
机译：本发明涉及制备（通式I）的疏水化的透明质酸盐的方法，并且进一步涉及将生物活性物质包封在疏水化的透明质酸盐的纳米胶束中的功能，所述纳米质纤体用作生物活性疏水性物质的载体。透明质酸盐的疏水化是通过透明质酸盐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盐形成。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酯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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