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Review
. 2022 Jul 7;23(14):7519.
doi: 10.3390/ijms23147519.

Bioavailability Improvement Strategies for Icariin and Its Derivates: A Review

Róbert Szabó  1 , Csaba Pál Rácz  2 , Francisc Vasile Dulf  1
Affiliations
Review

Bioavailability Improvement Strategies for Icariin and Its Derivates: A Review

Róbert Szabó et al. Int J Mol Sci. .

Abstract

In recent years, there has been considerable interest in icariin (ICA) and its derivates, icariside II (ICS) and icaritin (ICT), due to their wide range of potential applications in preventing cancer, cardiovascular disease, osteoporosis, delaying the effects of Alzheimer's disease, treating erectile dysfunction, etc. However, their poor water solubility and membrane permeability, resulting in low bioavailability, dampens their potential beneficial effects. In this regard, several strategies have been developed, such as pharmaceutical technologies, structural transformations, and absorption enhancers. All these strategies manage to improve the bioavailability of the above-mentioned flavonoids, thus increasing their concentration in the desired places. This paper focuses on gathering the latest knowledge on strategies to improve bioavailability for enhancing the efficacy of icariin, icariside II, and icaritin. We conclude that there is an opportunity for many further improvements in this field. To the best of our knowledge, no such review articles scoping the bioavailability improvement of icariin and its derivates have been published to date. Therefore, this paper can be a good starting point for all those who want to deepen their understanding of the field.

Keywords: bioavailability; complex formation; icariin; icariside II; icaritin; micelle; solubility improvement.

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Conflict of interest statement

The authors declare no conflict of interest.

Figures

Figure 1
Figure 1
The medicinal properties of icariin [49].
Figure 2
Figure 2
The molecular structure of icariin, icariside II, and icaritin.
Figure 3
Figure 3
Molecular structure of β-cyclodextrin.
Figure 4
Figure 4
Bioavailability improvement in the case of different techniques.
See this image and copyright information in PMC

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