Abstract Classic dendrimers are not used in many specific applications such as simultaneous loading of different drugs due to the existence of identical end groups. The possibility of designing the structure in dendrimers paves the way to synthesize more complicated dendrimers. This includes the creation of various types of peripheral groups on the surface of dendrimers to synthesize for example Janus dendrimers. Nowadays, three main methods are proposed for the synthesis of Janus dendrimers in which the high amount of conventional dendrimers is produced. The goal of this work is to develop a new method for synthesis of Janus dendrimers without production of conventional dendrimers. The present method has three main stages for the synthesis of Janus dendrimers including synthesis of 5th generation PPI dendrimer with cystamine core and hydrophobic surface, conversion of disulfide bonds to thiol group using a structure scission approach, and the formation of PAMAM hydrophilic dendrons with amine end groups. Different analyses including FT-IR, NMR, DLS, and GPC are used to prove the success of the synthesis route. Also, due to application of dendrimers in drug delivery including solubility improvement of hydrophobic drugs, Janus dendrimers are used to improve solubility of tetracycline and dexamethasone in presence of different generations of Janus dendrimers. Since the Janus dendrimers have both hydrophilic and hydrophobic ends, as well as having numerous terminal groups and numerous internal cavities, they have resulted in significant improvements in drug solubility. Also, solubility of the two hydrophobic drugs in water was increased by increasing concentration and generation of dendrimer.

中文翻译：

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两亲性 Janus 树枝状聚合物的合成及其在提高疏水性药物在水介质中的溶解度中的应用

摘要 由于存在相同的端基，经典的树枝状大分子没有用于许多特定的应用，例如同时装载不同的药物。在树枝状聚合物中设计结构的可能性为合成更复杂的树枝状聚合物铺平了道路。这包括在树枝状聚合物表面创建各种类型的外围基团以合成例如 Janus 树枝状聚合物。如今，提出了三种主要的方法来合成 Janus 树枝状大分子，其中产生大量的常规树枝状大分子。这项工作的目标是开发一种新方法来合成 Janus 树枝状大分子，而无需生产常规树枝状大分子。本方法合成 Janus 树枝状大分子包括三个主要阶段，包括合成具有胱胺核心和疏水表面的第 5 代 PPI 树枝状大分子，使用结构断裂方法将二硫键转化为硫醇基团，以及形成具有胺末端的 PAMAM 亲水树枝状大分子。组。包括 FT-IR、NMR、DLS 和 GPC 在内的不同分析用于证明合成路线的成功。此外，由于树枝状大分子在药物递送中的应用，包括提高疏水性药物的溶解度，因此在不同代的 Janus 树枝状大分子存在的情况下，Janus 树枝状大分子被用于提高四环素和地塞米松的溶解度。由于 Janus 树枝状大分子既有亲水端也有疏水端，还有许多端基和许多内腔，它们导致药物溶解度的显着改善。此外，两种疏水性药物在水中的溶解度随着树枝状大分子浓度和生成量的增加而增加。