Bioavailability Improvement Strategies for Icariin and Its Derivates: A Review

Szabó, Róbert; Rácz, Csaba; Dulf, Francisc Vasile

doi:10.3390/ijms23147519

Cited by 30 publications

(18 citation statements)

References 104 publications

(112 reference statements)

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“…Small amounts (0.25%) of water-soluble polymers and organic salts such as sodium salicylate, hydroxypropyl methylcellulose, sodium carboxymethyl cellulose, polyvinylpyrrolidone, polyethylene glycol 4000, sodium dodecyl sulfate, hexadimethrine bromide, tris(hydroxymethyl)aminomethane, sodium acetate or benzalkonium chloride were added to the complexation reaction. After work up and HPLC analysis, it was found that the complexation with addition of sodium dodecyl sulfate could increase icariin’s water solubility to 13.09 mg/mL, which is the best result obtained so far and is 654 times higher than that of the icariin ( Szabó et al, 2022 ). The inclusion rate and yield of icariin inclusion compound were obtained as 1.8% and 78.12% respectively, and the product was used for inclusion complex confirmation and in vitro and in vivo pharmacokinetic studies.…”

Section: Resultsmentioning

confidence: 89%

Improvement of solubility and pharmacokinetic profile of hepatoprotector icariin through complexation with HP-γ-cyclodextrin

Ding

Songyang³

et al. 2023

Front. Pharmacol.

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Icariin as a hepatoprotector from Herba epimedii can expand the cardiovascular and cerebral blood vessels, promote hematopoietic functions, enhance the immune system and show anti-liver tumor activities. However, its low solubility (0.02 mg/mL) limits its clinical applications as food and medical supplements. Through complexation with HP-γ-cyclodextrin by using a trace amount of water-soluble polymer, the water solubility of icariin was increased by 654 times, which is the best result to date for the water solubility study of icariin. In an in vitro pharmacokinetic study, the complexation increased the dissolution rate of icariin by 80 times, and the icariin complex can be 100% released in the first few minutes. Through complexation, in an in vivo dog pharmacokinetic study, the Cmax of icariin was increased about 5 times, the AUC0-120 was increased about 20 times and the clearance of icariin was changed from 11.17 L/h/kg to 0.65 L/h/kg. The half-life time was changed from 0.68 h to 6.38 h and the relative bioavailability was increased by nearly 20 times, indicating that less drug is needed for the same therapeutic effect by using the icariin complex, and the complex can be used as a potential potent hepatoprotector or anti-liver cancer drug.

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Section: Resultsmentioning

confidence: 89%

Improvement of solubility and pharmacokinetic profile of hepatoprotector icariin through complexation with HP-γ-cyclodextrin

Ding

Songyang³

et al. 2023

Front. Pharmacol.

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“…Notably, the impact of polyphenols in preventing drug resistance appears encouraging in oncology therapy [ 14 ]. Icariin is one of the main active ingredients of the Chinese botanical drug Epimedium, a well-researched anti-cancer agent [ 76 ]. Icariin induces apoptosis in TMX-resistant breast cancer cells and inhibits autophagy; thus, it is an ideal sensitizing agent.…”

Section: Natural Products Overcome Autophagy-mediated Tumor Drug Resi...mentioning

confidence: 99%

Focusing on the Role of Natural Products in Overcoming Cancer Drug Resistance: An Autophagy-Based Perspective

Yao

Feng

et al. 2022

Biomolecules

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Autophagy is a critical cellular adaptive response in tumor formation. Nutritional deficiency and hypoxia exacerbate autophagic flux in established malignancies, promoting tumor cell proliferation, migration, metastasis, and resistance to therapeutic interventions. Pro-survival autophagy inhibition may be a promising treatment option for advanced cancer. Furthermore, excessive or persistent autophagy is cytotoxic, resulting in tumor cell death. Targeted autophagy activation has also shown significant promise in the fight against tumor drug resistance. Several research groups have examined the ability of natural products (NPs) such as alkaloids, terpenoids, polyphenols, and anthraquinones to serve as autophagy inhibitors or activators. The data support the capacity of NPs that promote lethal autophagy or inhibit pro-survival autophagy from being employed against tumor drug resistance. This paper discusses the potential applications of NPs that regulate autophagy in the fight against tumor drug resistance, some limitations of the current studies, and future research needs and priorities.

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“…Icariin (ICA), an active component extracted from Epimedium species, has broad biological application prospects [ 2 ]. Numerous studies have shown that ICA and its metabolites can improve neuronal survival and function by reducing the production of extracellular amyloid beta peptide (Aβ) [ 3 ] and intracellular neurofibrillary tangles (NFTs) and inhibiting phosphodiesterase-5 activity [ 4 ].…”

Section: Introductionmentioning

confidence: 99%

Anti-Alzheimers molecular mechanism of icariin: insights from gut microbiota, metabolomics, and network pharmacology

Liu

Wang

et al. 2023

J Transl Med

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Background Icariin (ICA), an active ingredient extracted from Epimedium species, has shown promising results in the treatment of Alzheimer's disease (AD), although its potential therapeutic mechanism remains largely unknown. This study aimed to investigate the therapeutic effects and the underlying mechanisms of ICA on AD by an integrated analysis of gut microbiota, metabolomics, and network pharmacology (NP). Methods The cognitive impairment of mice was measured using the Morris Water Maze test and the pathological changes were assessed using hematoxylin and eosin staining. 16S rRNA sequencing and multi-metabolomics were performed to analyze the alterations in the gut microbiota and fecal/serum metabolism. Meanwhile, NP was used to determine the putative molecular regulation mechanism of ICA in AD treatment. Results Our results revealed that ICA intervention significantly improved cognitive dysfunction in APP/PS1 mice and typical AD pathologies in the hippocampus of the APP/PS1 mice. Moreover, the gut microbiota analysis showed that ICA administration reversed AD-induced gut microbiota dysbiosis in APP/PS1 mice by elevating the abundance of Akkermansia and reducing the abundance of Alistipe. Furthermore, the metabolomic analysis revealed that ICA reversed the AD-induced metabolic disorder via regulating the glycerophospholipid and sphingolipid metabolism, and correlation analysis revealed that glycerophospholipid and sphingolipid were closely related to Alistipe and Akkermansia. Moreover, NP indicated that ICA might regulate the sphingolipid signaling pathway via the PRKCA/TNF/TP53/AKT1/RELA/NFKB1 axis for the treatment of AD. Conclusion These findings indicated that ICA may serve as a promising therapeutic approach for AD and that the ICA-mediated protective effects were associated with the amelioration of microbiota disturbance and metabolic disorder. Graphical Abstract

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Bioavailability Improvement Strategies for Icariin and Its Derivates: A Review

Cited by 30 publications

References 104 publications

Improvement of solubility and pharmacokinetic profile of hepatoprotector icariin through complexation with HP-γ-cyclodextrin

Improvement of solubility and pharmacokinetic profile of hepatoprotector icariin through complexation with HP-γ-cyclodextrin

Focusing on the Role of Natural Products in Overcoming Cancer Drug Resistance: An Autophagy-Based Perspective

Anti-Alzheimers molecular mechanism of icariin: insights from gut microbiota, metabolomics, and network pharmacology

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