A Comparative Study of the Use of Mesoporous Carbon and Mesoporous Silica as Drug Carriers for Oral Delivery of the Water-Insoluble Drug Carvedilol

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.

Effective Targeting of Colon Cancer Cells with Piperine Natural Anticancer Prodrug Using Functionalized Clusters of Hydroxyapatite Nanoparticles

“…This observation can be explained by most Pip molecules being entrapped inside pores on the surface of HAPs. These results are in agreement with reports of loading drugs in mesoporous nanoparticles [30,31,63]. Changing the crystalline state of a water-insoluble drug to the non-crystalline state using mesoporous materials can enhance solubility, increasing the drug therapeutic activity [64].…”

High Surface Area Mesoporous Silica Nanoparticles with Tunable Size in the Sub-Micrometer Regime: Insights on the Size and Porosity Control Mechanisms

“…However, the control of particle size, specifically below 200 nm, remains challenging, due to the easy tendency of MSNs to aggregate. Indeed, MSN size regime between 50–200 nm, together with monodispersity, controlled pore size, shape and surface chemistry, represent essential features for biomedical application of MSNs as drugs and contrast agent vehicles [ 24 , 25 ]. Several studies have showed that efficiency of the cellular uptake and possibility to penetrate through the membranes/tissue are strongly dependent on particle size.…”

Exploiting Food-Grade Mesoporous Silica to Preserve the Antioxidant Properties of Fresh Olive Mill Wastewaters Phenolic Extracts

“…Moreover, ethanol can be easily and rapidly eliminated using rotary evaporation. The amount of phenolic extract to be loaded (phenolic extract:Syloid ® AL-1, 30:70, w / w ) was chosen on the basis of the values reported in the literature for different drugs and Syloid ® AL-1, and other mesoporous silicas having comparable surface area [ 26 , 32 , 33 ]. A theoretical loading of 30% ( w : w ) allows obtaining a final product where the phenolic extract is completely adsorbed and included in the pores of the mesoporous silica.…”