In this paper, we aim to create fully biodegradable glyconanoparticles formed via self-assembly of glycopolymers, comprising of biodegradable aliphatic polyester conjugated with mannose moiety. To accomplish the goal, a series of random copolymers comprised of poly(propargyl glycolide-co-lactide) were synthesized. Alkyne moiety of the poly (propargyl glycolide) component was then clicked with mannose ethyl azide to produce amphiphilic glycopolymers in good yield (60–75 %). The glycopolymers were then self-assembled to form glyconanoparticles of 15–23 nm size in dry state and 78–88 nm size in hydrated state (hydrodynamic diameter). The copolymers were characterized by NMR and FTIR, whereas the nanoparticles were thoroughly characterized by DLS, FESEM, and HR-TEM and explored for their lectin binding efficiency. Isothermal calorimetry (ITC) experiments suggest a stronger binding efficiency of glyconanoparticles towards mannose-specific lectin such as Concanavalin A, as compared to its corresponding glycopolymers (∼2 fold) and monomeric mannose unit (∼7-fold) as well. Moreover, curcumin was selected as the model drug to be encapsulated (∼76 % encapsulation efficiency) and released (74 % in 24 h) from the glyconanoparticles. Apart from these, excellent haemocompatibility, cell viability, and cellular uptake of the nanoparticles (more than 80 % cells showed uptake of the nanoparticles), further supported their potential as drug carriers having sugar as a targeting moiety.

中文翻译：

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甘露糖共轭生物可降解聚酯纳米载体的合成及其与伴刀豆球蛋白A的结合研究


在本文中，我们的目标是通过糖聚合物的自组装形成完全可生物降解的糖纳米粒子，该糖聚合物由与甘露糖部分缀合的可生物降解的脂肪族聚酯组成。为了实现这一目标，合成了一系列由聚（炔丙乙交酯-丙交酯）组成的无规共聚物。然后，聚（炔丙乙交酯）组分的炔部分与甘露糖乙基叠氮化物点击，以良好的产率（60-75%）生产两亲性糖聚合物。然后，糖聚合物自组装形成干燥状态下尺寸为 15-23 nm 和水合状态下尺寸为 78-88 nm（流体动力学直径）的糖纳米颗粒。共聚物通过 NMR 和 FTIR 进行表征，而纳米颗粒则通过 DLS、FESEM 和 HR-TEM 进行彻底表征，并探索其凝集素结合效率。等温量热法 (ITC) 实验表明，与相应的糖聚合物（~2 倍）和单体甘露糖单元（~7 倍）相比，糖纳米粒子对甘露糖特异性凝集素（如刀豆球蛋白 A）具有更强的结合效率。此外，选择姜黄素作为模型药物，从糖纳米颗粒中封装（~76% 封装效率）并释放（24 小时内释放 74%）。除此之外，纳米颗粒优异的血液相容性、细胞活力和细胞摄取（超过80%的细胞显示出纳米颗粒的摄取）进一步支持了它们作为以糖为靶向部分的药物载体的潜力。