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A Eu3+/Gd3+-EDTA-doped structurally controllable hollow mesoporous carbon for improving the oral bioavailability of insoluble drugs and in vivo tracing

机译:Eu3 + / Gd3 + -EDTA掺杂的结构可控空心中孔碳,用于改善不溶性药物的口服生物利用度和体内示踪

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A structurally controllable fluorescence-labeled hollow mesoporous carbon (HMC) was simply prepared to improve the oral bioavailability of insoluble drugs and further trace their delivery process in vivo. The hollow structure was derived from an inverse replica process using mesoporous silica as a template and the fluorescent label was prepared by doping the carboxylated HMC with a confinement of Eu3+/Gd3+-EDTA. The physicochemical properties of the composites were systematically characterized by transmission electron microscopy, Fourier transform infrared spectroscopy and photoluminescence spectra tests prior to studying their effects on drug-release behavior and biodistribution. As a result, the thickness of the carrier's shell was adjusted from 70 nm to 130 nm and the maximum drug loading was up to 73.6%. The model drug carvedilol (CAR) showed sustained release behavior compared to CAR commercial capsules, and the dissolution rate slowed down as the shells got thicker. AUC(0-48h) and Tmax were enlarged 2.2 and 6.5 fold, respectively, which demonstrated that oral bioavailability was successfully improved. Bioimaging tests showed that the novel carbon vehicle had a long residence time in the gastrointestinal tract. In short, the newly designed HMC is a promising drug carrier for both oral bioavailability improvement and in vivo tracing.
机译:简单地制备结构可控制的荧光标记的空心中孔碳(HMC),以提高不溶性药物的口服生物利用度,并进一步追踪其体内递送过程。中空结构源自以中孔二氧化硅为模板的逆复制过程,荧光标记是通过将羧基化的HMC掺入Eu3 + / Gd3 + -EDTA限制而制得的。在研究它们对药物释放行为和生物分布的影响之前,通过透射电子显微镜,傅立叶变换红外光谱和光致发光光谱测试系统地表征了复合材料的理化性质。结果,将载体壳的厚度从70nm调节至130nm,并且最大载药量高达73.6%。与CAR商业胶囊相比,模型药物卡维地洛(CAR)表现出持续释放的特性,并且随着壳层的增厚,溶出度减慢。 AUC(0-48h)和Tmax分别提高了2.2倍和6.5倍,这表明口服生物利用度得到了成功的改善。生物成像测试表明,新型碳载体在胃肠道中的停留时间很长。简而言之,新设计的HMC是改善口服生物利用度和体内追踪的有前途的药物载体。

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