Abstract
Encapsulation of poorly water-soluble drugs into mesoporous materials (e.g. silica) has evolved as a favorable strategy to improve drug solubility and bioavailability. Several techniques (e.g. spray drying, solvent evaporation, microwave irradiation) have been utilized for the encapsulation of active pharmaceutical ingredients (APIs) into inorganic porous matrices. In the present work, a novel chalcone (KAZ3) with anticancer properties was successfully synthesized by Claisen-Schmidt condensation. KAZ3 was loaded into mesoporous (SBA-15 and MCM-41) and non-porous (fumed silica, FS) materials via two techniques; electrohydrodynamic atomization (EHDA) and solvent impregnation. The effect of both loading methods on the physicochemical properties of the particles (e.g. size, charge, entrapment efficiency, crystallinity, dissolution and permeability) was investigated. Results indicated that EHDA technique can load the active in a complete amorphous form within the pores of the silica particles. In contrast, reduced crystallinity (~79%) was obtained for the solvent impregnated formulations. EHDA engineered formulations significantly improved drug dissolution up to 30-fold, compared to the crystalline drug. Ex vivo studies showed EHDA formulations to exhibit higher permeability across rat intestine than their solvent impregnated counterparts. Cytocompatibility studies on Caco-2 cells demonstrated moderate toxicity at high concentrations of the anticancer agent. The findings of the present study clearly show the immense potential of EHDA as a loading technique for mesoporous materials to produce poorly water-soluble API carriers of high payload at ambient conditions. Furthermore, the scale up potential in EHDA technologies indicate a viable route to enhance drug encapsulation and dissolution rate of loaded porous inorganic materials.
Highlights
Cancer is a deleterious disease that accounts for a high annual global mortality rate
This decoration aimed to decrease the reactivity of α, β-unsaturated carbonyl group decreasing their possible interactions with biological molecules and the potential of adverse effects [7]
The purity of the product was determined by thin layer chromatography (TLC) and elemental analysis
Summary
Cancer is a deleterious disease that accounts for a high annual global mortality rate. Mesoporous silica materials (pore size 2–50 nm) have been explored as targeted [2,25] responsive [26] and controlled [27,28] drug delivery systems, because of their favorable features, such as a stable ordered porous network, accessible silanol groups, high surface area as well as uniform and tuneable pore and particle size [29] They are considered as promising API carriers which improve the dissolution rate and oral bioavailability of poorly water-soluble drugs [21,30] by drug amorphization [19]. The potential for enhanced drug loading, increased stability of the drug in the amorphous state, displaying improved dissolution and permeability profiles is demonstrated
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