Abstract

In this work, rutin (RUT)–β-cyclodextrin (β-CD) inclusion complexes are prepared by Supercritical AntiSolvent (SAS) precipitation. Well-defined composite microparticles are obtained at guest:host ratios equal to 1:2 and 1:1 mol:mol. The dimensions of composite particles range between 1.45 ± 0.88 µm and 7.94 ± 2.12 µm. The formation of RUT–β-CD inclusion complexes has been proved by different analyses, including Fourier transform infrared spectroscopy, Differential Scanning Calorimetry, X-ray diffraction, and UV-vis spectroscopy. The dissolution tests reveal a significant improvement in the release rate of RUT from inclusion complexes. Indeed, compared to the unprocessed RUT, the dissolution rate is about 3.9 and 2.4 times faster in the case of the complexes RUT–β-CD 1:2 and 1:1 mol:mol, respectively. From a pharmaceutical/nutraceutical point of view, CD-based inclusion complexes allow the reduction of the polymer amount in the SAS composite formulations.

Highlights

  • Rutin (RUT) is a flavonoid, which is a group of polyphenols, defined as vitaminP

  • The high-pressure pump P2 permits to feed the liquid solution, which consists of the solutes (RUT, β-CD) solubilized in the liquid solvent (DMSO); in detail, it is injected through a 100 μm internal diameter stainless-steel nozzle

  • The indicated flow rates were chosen to operate with CO2 molar fractions approximately equal to 0.98 at the selected temperature; i.e., on the right of the Mixture Critical Point (MCP) of the binary system CO2 –DMSO to assure the supercritical mixture conditions [40,41]

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Summary

Introduction

Rutin (RUT) is a flavonoid, which is a group of polyphenols, defined as vitamin. The papers focused on obtaining inclusion complexes containing rutin are not exhaustive and fully satisfactory; this can be linked to the drawbacks of the used traditional techniques: multistage processing, possible thermal degradation of the encapsulated active principle, high solvent residues in the product, and attainment of composites with irregular morphology/shape [14,22,23,24]. These limits can be overcome by employing supercritical carbon dioxide (scCO2 )-based technologies [25,26,27]; the various techniques can be classified according to the role played by scCO2 with respect to the active principle. The final purpose is to propose alternative formulations or supplements, exploiting the numerous beneficial properties of the natural active compound and improving its therapeutic efficacy

Materials and Methods
SAS Apparatus and Procedure
Analytical
Methods
Experimental Results and Discussion
Volumetric
The XRD patterns of pure RUT and β‐CD show the crystallin
Conclusions and Perspectives
Full Text
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