A Comparative Study of the Use of Mesoporous Carbon and Mesoporous Silica as Drug Carriers for Oral Delivery of the Water-Insoluble Drug Carvedilol
2019
Cuiyan Han | Haitao Huang | Yan Dong | Xiaoyu Sui | Baiyu Jian | Wenquan Zhu
Mesoporous carriers have been extensively applied to improve the dissolution velocity and bioavailability of insoluble drugs. The goal of this work was to compare the drug-loading efficiency (LE) and drug-dissolution properties of mesoporous silica nanoparticles (MSN) and mesoporous carbon nanoparticles (MCN) as drug vectors oral delivery of water-insoluble drugs. For this purpose, MSN and MCN with similar particle size, surface area, and mesoporous diameter were prepared to precisely evaluate the effects of different textures on the drug-loading and dissolution behavior of insoluble drugs. Carvedilol (CAR), a Bio-pharmaceutic Classification System (BCS) class II drug, was loaded in the MSN and MCN by the solvent adsorption method and solvent evaporation method with different carrier&ndash:drug ratios. The carboxylated MCN (MCN&ndash:COOH) had a higher LE for CAR than MSN for both the two loading methods due to the strong adsorption effect and &pi:&ndash:&pi: stacking force with CAR. In vitro drug dissolution study showed that both MSN and MCN-COOH could improve the dissolution rate of CAR compared with the micronized CAR. In comparison to MSN, MCN-COOH displayed a slightly slower dissolution profile, which may be ascribed to the strong interaction between MCN-COOH and CAR. Observation of cell cytotoxicity and gastrointestinal mucosa irritation demonstrated the good biocompatibility of both MSN and MCN&ndash:COOH. The present study encourages further research of different carriers to determine their potential application in oral administration.
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