Abstract
Diosmin (DSN) exhibits poor water solubility and low bioavailability. Although nanocrystals (NCs) are successful for improving drug solubility, they may undergo crystal growth. Therefore, DSN NCs were prepared, employing sonoprecipitation utilizing different stabilizers. The optimum stabilizer was combined with chitosan (CS) as an electrostatic stabilizer. NCs based on 0.15% w/v poloxamer 188 (PLX188) as a steric stabilizer and 0.04% w/v CS were selected because they showed the smallest diameter (368.93 ± 0.47 nm) and the highest ζ-potential (+40.43 ± 0.15 mV). Mannitol (1% w/v) hindered NC enlargement on lyophilization. FT-IR negated the chemical interaction of NC components. DSC and XRD were performed to verify the crystalline state. DSN dissolution enhancement was attributed to the nanometric rod-shaped NCs, the high surface area, and the improved wettability. CS insolubility and its diffusion layer may explain controlled DSN release from CS-PLX188 NCs. CS-PLX188 NCs were more stable than PLX188 NCs, suggesting the significance of the combined electrostatic and steric stabilization strategies. The superiority of CS-PLX188 NCs was indicated by the significantly regulated biomarkers, pathological alterations, and inducible nitric oxide synthase (iNOS) expression of the hepatic tissue compared to DSN suspension and PLX188 NCs. Permeation, mucoadhesion, and cellular uptake enhancement by CS may explain this superiority.
Highlights
70–90% of active pharmaceutical compounds encounter poor water solubility, which diminishes their bioavailability [1]
A uniform particle size distribution was verified by polydispersity index (PDI) ≤ 0.55 ± 0.02
The stabilizer concentration was critical. The increase in their concentrations from 0.1% w/v to 0.15% w/v resulted in smaller nanoparticles
Summary
70–90% of active pharmaceutical compounds encounter poor water solubility, which diminishes their bioavailability [1]. Nanocrystallization is a promising tool for enhancing the solubility of many drugs due to the high loading efficiency, the cost effectiveness, and the manufacturing simplicity, which can encourage large-scale production [2]. They can be used in the form of capsules, pellets, tablets, and nanosuspensions [3]. NCs can be prepared by either top-down or bottom-up techniques [5,6]. Nanoprecipitation as a bottom-up technique is simple, rapid, cost-effective, and suitable for scaling up [8]. Nanoprecipitation can provide smaller NCs [6]. Nanoprecipitation has some shortcomings, such as lower drug loading and large amount of solvent that should be removed in the processing [9]
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