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Graphene oxide as a potential drug carrier - Chemical carrier activation, drug attachment and its enzymatic controlled release.
Biomaterials Advances ( IF 5.5 ) Pub Date : 2020-06-24 , DOI: 10.1016/j.msec.2020.111240
Anna Trusek 1 , Edward Kijak 2 , Ludomira Granicka 3
Affiliation  

Graphene oxide (GO), due to its properties, such as nanometric dimensions, large specific surface area, and biocompatibility, can be used as a carrier in controlled drug release systems. The method of its chemical activation before drug molecules binding was elaborated. Doxorubicin (DOX), an anticancer drug, was attached to the surface of GO via the Gly-Gly-Leu linker. Approximately 3.07 · 1020 molecules of the tripeptide were attached to 1 g of GO and subsequently almost the same number of DOX molecules. GO was suspended inside a sol surrounded by a thin porous membrane. The bound DOX was effectively released using thermolysin, an enzyme cleaving peptide bonds between Gly and Leu inside the linker structure. The membrane, as the shell was responsible for keeping enzyme molecules in their native form and GO flakes inside the carrier, simultaneously allowed the released drug molecules to diffuse outside. The rate of drug release was described as a function of the enzyme concentration and mass of DOX expressed on carrier volume; thus, the daily dose and length of the therapy can be controlled. Studies involving the cell line of mice fibrosarcoma WEHI 164 have shown that the prepared carrier itself is not toxic and only the introduction of DOX-releasing enzyme into it causes cell death.



中文翻译:

氧化石墨烯作为潜在的药物载体-化学载体活化,药物附着及其酶促控制释放。

由于其性质,例如纳米尺寸,大的比表面积和生物相容性,氧化石墨烯(GO)可用作受控药物释放系统中的载体。阐述了药物分子结合前的化学活化方法。阿霉素(DOX)是一种抗癌药物,通过Gly-Gly-Leu接头连接到GO的表面。约3.07·10 20将三肽的两个分子连接到1 g的GO上,然后将其连接到几乎相同数量的DOX分子上。GO悬浮在被多孔薄膜包围的溶胶中。使用嗜热菌素可以有效释放结合的DOX,嗜热菌素是一种在连接子结构内部的Gly和Leu之间裂解肽键的酶。膜作为外壳负责将酶分子保持其天然形式,而GO薄片则位于载体内部,同时允许释放的药物分子向外扩散。药物释放速率描述为酶浓度和载体体积上表达的DOX质量的函数;因此,可以控制每日剂量和治疗时间。

更新日期:2020-06-24
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