Parshad Badri, Kumari Meena, Achazi Katharina, Bӧttcher Christoph, Haag Rainer, Sharma Sunil K
Department of Chemistry, University of Delhi, Delhi 110 007, India.
Institut für Chemie und Biochemie, Freie Universität Berlin, Takustraße 3, Berlin 14195, Germany.
Polymers (Basel). 2016 Aug 18;8(8):311. doi: 10.3390/polym8080311.
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 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.
在具有不同骨架的两亲性聚合物中，含氟结构因其独特的分离特性以及自组装成离散超分子实体的能力而备受关注。在此，我们通过将疏水性烷基/全氟烷基链和亲水性聚甘油[G2.0]树枝状分子接枝到共聚物支架上合成了两亲性共聚物，该共聚物支架本身是通过聚[乙二醇双(羧甲基)醚]二乙酯和2-叠氮基丙烷-1,3-二醇的酶促聚合制备的。然后，使用姜黄素和地塞米松药物，对所得含氟聚合物及其烷基链类似物在超分子聚集行为、增溶能力、转运潜力和释放曲线方面进行了比较。对包封的姜黄素在有/无水解酶脂肪酶（CAL-B）存在下孵育的释放曲线研究表明，与烷基链类似物相比，在没有酶的情况下，药物在全氟烷基链接枝的聚合物纳米结构中能更好地稳定长达12天。尽管在与脂肪酶孵育时，含氟和非含氟体系在12天内姜黄素的释放量均高达90%，但在含氟聚合物中观察到相对较快的释放。在含氟聚合物（100μg/mL）水溶液中，HeLa细胞的活力高达95%，证明了它们具有优异的细胞相容性。
