Abstract
The aim of our study was to obtain rutoside (RUT) inclusion complexes in β-cyclodextrin (β-CD) and in hydroxypropyl-β-cyclodextrin (HP-β-CD), in a 1:1 molar ratio, using the lyophilization method of complexation in solution. The complexes were confirmed and characterized, in comparison with the raw materials and their simple physical mixtures, by SEM, DSC, and FT-IR analyses. The antioxidant activity of the compounds was assessed by using the 2,2-diphenyl-1-picryl-hydrazyl (DPPH) and 2’-azino-bis(3-ethylbenzothiazolin-6-sulfonic) acid (ABTS) radicals, determining the radical scavenging activity, and by ferric reducing antioxidant power (FRAP) assay. The results revealed superior antioxidant ability for the inclusion complexes towards rutoside alone. The inclusion complexes were used as active ingredients in formulations of immediate-release tablets. The preformulation studies were performed on the powders for direct compression obtained after mixing the active ingredients with the excipients (Avicel PH 102, Polyplasdone XL-10, magnesium stearate, and talc). The materials were assessed for particle size, flowability, compressibility, and moisture content, establishing they are suitable for a direct compression process. The tablets were characterized regarding their pharmaco-technical properties and the results proved that the formulations lead to high-quality delivery systems, showing a good mechanical resistance with a low friability, excellent disintegration times, and satisfying dissolution rate. The performances were very similar for both formulations and the physico-mechanical properties of the tablets are not influenced by type of the used cyclodextrin, but the RUT- HP-β-CD tablets presented a higher dissolution rate.
Highlights
IntroductionRutoside (RUT) ( known as rutin, quercetin-3-O-glucoside, and sophorin) is a natural flavonoid glycoside that has quercetin as the aglycone part, and a disaccharide, rutinose [α-L-rhamnopyranosyl-(1→6)-β-D-glucopyranose], as the glucidic part
Rutoside (RUT) is a natural flavonoid glycoside that has quercetin as the aglycone part, and a disaccharide, rutinose [α-L-rhamnopyranosyl-(1→6)-β-D-glucopyranose], as the glucidic part
The results proved that both cyclodextrins, β-CD and HP-β-CD, do not possess antioxidant capacities, but they have a significant influence on the ABTS radical scavenging activity of rutoside
Summary
Rutoside (RUT) ( known as rutin, quercetin-3-O-glucoside, and sophorin) is a natural flavonoid glycoside that has quercetin as the aglycone part, and a disaccharide, rutinose [α-L-rhamnopyranosyl-(1→6)-β-D-glucopyranose], as the glucidic part. Beyond its scientifically proven effectiveness, rutoside processing in different pharmaceutical forms is still hard to be made, due to its low oral absorption and bioavailability, as a result of poor solubility and chemical instability [11,12]. A lot of studies were aimed at enhancing the stability, solubility, absorbability, and bioavailability of rutoside, by using rutoside derivates, particle size reduction, the use of surfactants, or sugar coating [13,14,15]. A facile and effective method for increasing the solubility, stability, and antioxidant activity of rutoside is its inclusion in the cyclodextrins cavities by forming inclusion complexes [16,17,18]. Cyclodextrins are cyclic oligosaccharides able to include various molecules in their internal hydrophobic cavity, frequently used to improve the water solubility of encapsulated ingredients due to their hydrophilic external surface [19]
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