生物素化ph响应型糖共聚物的制备及其控制硼替佐米释放的纳米递送载体

I. Abdalla, Zhongli Niu, B. Sun, X. Jiang, Meifang Zhu
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摘要

为了开发生物素化的ph响应型糖共聚物并研究其作为抗癌药物纳米载体的性能,合成了溴端生物素,然后通过原子转移自由基聚合(ATRP)引发d -氨基甲基丙烯酸乙酯(GAMA)和2-(二乙胺)甲基丙烯酸乙酯(DEA)单体的聚合。采用嵌段和随机结构分别制备了两种具有相似聚合度(DP)链段的生物素化ph响应共聚物Biotin-P(GAMA- b - dea)和Biotin-P(GAMA- co - dea)。表征了糖共聚物的化学组成和自组装行为。结果表明,嵌段共聚物在水介质中自组装成含有PGAMA壳和PDEA核的核壳结构,直径为28 nm,而无规嵌段共聚物在pH 7.4以上仍保持水溶性。两种糖共聚物均具有BTZ的负载能力,包封效率(EE %)和负载量(LC %)分别为83.7%和8.4%、78.7%和7.9%,且在pH 7.4条件下,24 h的累积释放量分别保持在20%和26%的低常数。该研究有望为开发具有优异生物相容性的新型智能药物载体体系提供参考。
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Preparation of Developing Biotinylated PH-Responsive Glycopolymers as Delivery Nanocarriers for Controlling Release of Bortezomib
To develop biotinylated pH-responsive glycopolymers and investigate their performances as anticancer drug delivery nanocarriers, bromide-terminated biotin was synthesized and then used to initiate the polymerization of D-gluconamido ethyl methacrylate (GAMA) and 2-(diethylamino)ethyl methacrylate (DEA) monomers via atom transfer radical polymerization (ATRP). Two biotinylated pH-responsive copolymers with similar degree polymerization (DP) chain segments, Biotin-P(GAMA- b -DEA) and Biotin-P(GAMA- co -DEA), were prepared by block or random architectures, respectively. The chemical compositions and self-assembly behavior of glycopolymers were characterized. The results show that the block glycopolymer self- assembles in water medium into core-shell structure assembly containing PGAMA shell and PDEA core with the 28 nm in diameter, while the random glycopolymer remains water-soluble state above pH 7.4. Both glycopolymers possess the loading ability of the BTZ with encapsulation efficiency (EE %) and loading capacity (LC %) of 83.7% and 8.4%, 78.7% and 7.9%, and the release behavior was kept at low constants with 20% and 26% cumulative amount even after 24 hours at pH 7.4, respectively. The study is expected to give the light to the development of new intelligent drug carrier system with excellent biological compatibility.
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