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均一介孔碳作为载体用于疏水性药物及其细胞毒性研究。

Uniform mesoporous carbon as a carrier for poorly water soluble drug and its cytotoxicity study.

机构信息

Department of Pharmaceutics, Shenyang Pharmaceutical University, Shenyang, China.

出版信息

Eur J Pharm Biopharm. 2012 Apr;80(3):535-43. doi: 10.1016/j.ejpb.2011.12.002. Epub 2011 Dec 13.

Abstract

In this study, uniform mesoporous carbon spheres (UMCS) with 3-D pore system and fibrous ordered mesoporous carbon (FOMC) with 2-dimensional hexagonal mesoporous structure were studied as drug carriers for oral drug delivery system. Lovastatin (LOV), which has low water solubility, was chosen as a model drug. Drug release rate and degree of drug loading of UMCS and FOMC were compared. The effects of different pore channel structures and pore sizes on LOV uptake and release were systematically investigated. Cytotoxicity of UMCS and FOMC on human colon carcinoma (Caco-2) cells were also studied. The results indicate that UMCS has a higher degree of drug loading (up to 36.26% drug weight/total weight) compared with FOMC. The dissolution rate of LOV from UMCS was found to be markedly increased compared with pure crystalline LOV, and the dissolution rate of LOV from FOMC was relatively sustained compared with UMCS, and both UMCS and FOMC exhibited a weak cytotoxicity at tested concentrations (10-800 μg/ml).

摘要

在这项研究中,我们研究了具有 3D 孔系统的均一介孔碳球(UMCS)和具有 2D 六方介孔结构的纤维有序介孔碳(FOMC),它们可作为口服药物传递系统的药物载体。洛伐他汀(LOV)具有低水溶性,被选为模型药物。比较了 UMCS 和 FOMC 的药物释放速率和载药量。系统研究了不同的孔道结构和孔径对 LOV 摄取和释放的影响。还研究了 UMCS 和 FOMC 对人结肠癌细胞(Caco-2)的细胞毒性。结果表明,UMCS 的载药量(高达 LOV 重量/总重量的 36.26%)高于 FOMC。与纯结晶 LOV 相比,UMCS 中 LOV 的溶解速率明显增加,而 FOMC 中 LOV 的溶解速率与 UMCS 相比相对稳定,并且在测试浓度(10-800μg/ml)下,UMCS 和 FOMC 均表现出较弱的细胞毒性。

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