Department of Pharmaceutics, School of Pharmacy, Shenyang Pharmaceutical University, 103 Wenhua Road, Shenyang, 110016, People's Republic of China.
Nanotechnology. 2016 Aug 5;27(31):315101. doi: 10.1088/0957-4484/27/31/315101. Epub 2016 Jun 23.
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 Eu(3+)/Gd(3+)-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. AUC0-48h 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.
一种结构可控的荧光标记中空介孔碳（HMC）被简单制备，以提高难溶性药物的口服生物利用度，并进一步追踪其在体内的递药过程。中空结构源自介孔硅模板的反复制过程，荧光标记是通过将羧基化的 HMC 掺杂 Eu(3+)/Gd(3+)-EDTA 来制备的。在研究其对药物释放行为和体内分布的影响之前，通过透射电子显微镜、傅里叶变换红外光谱和荧光光谱测试对复合材料的理化性质进行了系统表征。结果表明，载体壳的厚度可从 70nm 调节至 130nm，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）表现出持续释放行为，且随着壳层变厚，溶解速率减慢。AUC0-48h 和 Tmax 分别扩大了 2.2 倍和 6.5 倍，表明口服生物利用度得到了成功提高。生物成像测试表明，新型碳载体在胃肠道中有较长的停留时间。总之，新设计的 HMC 是一种有前途的药物载体，可用于提高口服生物利用度和体内追踪。
