Abstract
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–drug ratios. The carboxylated MCN (MCN–COOH) had a higher LE for CAR than MSN for both the two loading methods due to the strong adsorption effect and π–π 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–COOH. The present study encourages further research of different carriers to determine their potential application in oral administration.
Highlights
With the development of high–throughput screening technology, many new chemical drugs have been developed [1,2,3]
The MCM–48-type mesoporous silica nanoparticles (MSN) were prepared using with uniform particle size and highly mesopores shown in the transmission electron cetyltrimethylammonium bromide (CTAB)ordered as a template and F127 as a dispersion stabilizer
These results indicated that the MSN had similar SBET, VP, and pore size distribution (Pd) values when compared with small angle X-ray scattering (SAXS) pattern of MSN; (D) Nitrogen adsorption/desorption isotherms
Summary
With the development of high–throughput screening technology, many new chemical drugs have been developed [1,2,3]. It has been reported that more than 40% of new active substances cannot be used clinically because of their poor water solubility, resulting in low oral bioavailability and problems with oral absorption [4,5,6,7,8]. In order to transform more insoluble candidate compounds into new therapeutic drugs and maximize their efficacy, enhancing the solubility and bioavailability of these drugs is an important scientific problem that urgently needs to be solved. It is well known that more than one-third of candidate compounds are insoluble in aqueous solution, which might lead to poor oral absorption in the gastrointestinal (GI) tract [4]. The water-insoluble drugs which belong to the Bio-pharmaceutic Classification System (BCS) class II have the characteristics of high permeability and low solubility. The dissolution of water insoluble drugs in the GI tract
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