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用于局部应用的药物包封与释放的糖连接三唑两亲分子超分子凝胶。

Supramolecular gels from sugar-linked triazole amphiphiles for drug entrapment and release for topical application.

作者信息

Sharma Komal, Joseph Jojo P, Sahu Adarsh, Yadav Narender, Tyagi Mohit, Singh Ashmeet, Pal Asish, Kartha K P Ravindranathan

机构信息

Department of Medicinal Chemistry, National Institute of Pharmaceutical Education and Research (NIPER) S. A. S. Nagar Punjab-160062 India

Institute of Nano Science and Technology Phase 10, Sector 64 Mohali Punjab-160062 India

出版信息

RSC Adv. 2019 Jun 27;9(34):19819-19827. doi: 10.1039/c9ra02868d. eCollection 2019 Jun 19.

Abstract

A simple molecular framework obtained by cross-linking a hydrophobic chain with ,- and ,-tetritol by the copper-catalysed azide-alkyne cycloaddition reaction is found to serve as an excellent bioisostere for self-assembly. The hexadecyl-linked triazolyl tetritol composite spontaneously self-assembles in -hepane and methanol to form hierarchical organogels. Microscopic analyses and X-ray diffraction studies demonstrate eventual formation of nanotubes through lamellar assembly of the amphiphiles. A rheological investigation shows solvent-dictated mechanical properties that obey power law behavior similar to other low molecular weight gelators (LMOGs). The gel network was then utilized for the entrapment of drugs ibuprofen and 5-fluorouracil, with tunable mechanical behaviour under applied stress. The differential release profiles of the drugs over a period of a few hours as a result of the relative spatio-temporal location in the supramolecular network can be utilized for topical formulations.

摘要

通过铜催化的叠氮化物-炔烃环加成反应将疏水链与丙三醇和丁四醇交联得到的一个简单分子框架,被发现可作为用于自组装的优异生物电子等排体。十六烷基连接的三唑基丁四醇复合物在正庚烷和甲醇中自发自组装形成分级有机凝胶。显微镜分析和X射线衍射研究表明,两亲物通过层状组装最终形成纳米管。流变学研究表明,其溶剂决定的机械性能遵循与其他低分子量凝胶剂(LMOG)类似的幂律行为。然后将凝胶网络用于包封药物布洛芬和5-氟尿嘧啶,在施加应力下具有可调的机械行为。由于药物在超分子网络中的相对时空位置,在几个小时内的药物差异释放曲线可用于局部制剂。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a24c/9065371/3ae979c9471d/c9ra02868d-s1.jpg

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