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Chemo-Enzymatic Synthesis of Perfluoroalkyl-Functionalized Dendronized Polymers as Cyto-Compatible Nanocarriers for Drug Delivery Applications

机译:化学-酶促合成全氟烷基官能化的树枝状聚合物作为细胞相容性纳米载体的药物输送应用。

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摘要

Among amphiphilic polymers with diverse skeletons, fluorinated architectures have attracted significant attention due to their unique property of segregation and self-assembly into discrete supramolecular entities. Herein, we have synthesized amphiphilic copolymers by grafting hydrophobic alkyl/perfluoroalkyl chains and hydrophilic polyglycerol [G2.0] dendrons onto a co-polymer scaffold, which itself was prepared by enzymatic polymerization of poly[ethylene glycol bis(carboxymethyl) ether]diethylester and 2-azidopropan-1,3-diol. The resulting fluorinated polymers and their alkyl chain analogs were then compared in terms of their supramolecular aggregation behavior, solubilization capacity, transport potential, and release profile using curcumin and dexamethasone drugs. The study of the release profile of encapsulated curcumin incubated with/without a hydrolase enzyme Candida antarctica lipase (CAL-B) suggested that the drug is better stabilized in perfluoroalkyl chain grafted polymeric nanostructures in the absence of enzyme for up to 12 days as compared to its alkyl chain analogs. Although both the fluorinated as well as non-fluorinated systems showed up to 90% release of curcumin in 12 days when incubated with lipase, a comparatively faster release was observed in the fluorinated polymers. Cell viability of HeLa cells up to 95% in aqueous solution of fluorinated polymers (100 μg/mL) demonstrated their excellent cyto-compatibility.
机译:在具有不同骨架的两亲聚合物中,氟化结构由于其独特的分离和自组装成离散的超分子实体的特性而受到了广泛的关注。本文中,我们通过将疏水性烷基/全氟烷基链和亲水性聚甘油[G2.0]树突接枝到共聚物支架上合成了两亲共聚物,该共聚物支架本身是通过聚乙二醇双(羧甲基醚)二乙基酯和2-叠氮基-1,3-二醇。然后,使用姜黄素和地塞米松药物比较所得的氟化聚合物及其烷基链类似物的超分子聚集行为,增溶能力,转运潜力和释放曲线。对与/不与水解酶南极假丝酵母脂肪酶(CAL-B)一起孵育的胶囊化姜黄素释放曲线的研究表明,与不存在酶的情况相比,该药物在无酶的全氟烷基链接枝聚合物纳米结构中的稳定性要好于12天。其烷基链类似物。尽管与脂肪酶一起孵育时,氟化体系和非氟化体系在12天内都显示姜黄素释放高达90%,但在氟化聚合物中观察到了相对较快的释放。在含氟聚合物(100μg/ mL)的水溶液中,高达95%的HeLa细胞的细胞生存能力证明了其优异的细胞相容性。

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