Effect of β-cyclodextrin complexation on solubility and enzymatic hydrolysis rate of icariin

Cui, Li; Zhang, Zhenhai; Sun, E; Jia, Xiao‐Bin; Qian, Qian

doi:10.4103/0976-9668.107291

Cited by 14 publications

(3 citation statements)

References 21 publications

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“…To the best of our knowledge, this ICA-PG exhibits a stronger solubilizing power to ICA than any other in the current report. For example, the solubility of ICA in the β-cyclodextrin inclusion complex is only 525.6 μg ml −1 , while that of the bare ICA is 14.6 μg ml −1 , 33 which is only about 0.61% of the values recorded in our study. It is widely accepted that solubility is one of the important parameters for achieving the desired (anticipated) pharmacological response.…”

Section: Discussioncontrasting

confidence: 72%

Simple and novel icariin-loaded pro-glycymicelles as a functional food: physicochemical characteristics, in vitro biological activities, and in vivo experimental hyperlipidemia prevention evaluations

Cui,

Wang,

Zhou

et al. 2023

Food Funct.

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Section: Discussioncontrasting

confidence: 72%

Simple and novel icariin-loaded pro-glycymicelles as a functional food: physicochemical characteristics, in vitro biological activities, and in vivo experimental hyperlipidemia prevention evaluations

Cui,

Wang,

Zhou

et al. 2023

Food Funct.

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“…We must realize that the oral bioavailability rate is only 12.02% for 1 . Studies have shown the addition of cyclodextrins (CDs) to ICA can result in a vast increase in its water solubility, consequently achieving considerably better bioavailability ( Cui et al, 2013 ; Jin et al, 2013 ). The degradation of ICA into ICS in vivo promotes ICA absorption ( Cheng et al, 2015 ).…”

Section: Pharmacological Inhibition Of Ferroptosis For Treating Cardi...mentioning

confidence: 99%

Targeting ferroptosis as a promising therapeutic strategy to treat cardiomyopathy

et al. 2023

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Cardiomyopathies are a clinically heterogeneous group of cardiac diseases characterized by heart muscle damage, resulting in myocardium disorders, diminished cardiac function, heart failure, and even sudden cardiac death. The molecular mechanisms underlying the damage to cardiomyocytes remain unclear. Emerging studies have demonstrated that ferroptosis, an iron-dependent non-apoptotic regulated form of cell death characterized by iron dyshomeostasis and lipid peroxidation, contributes to the development of ischemic cardiomyopathy, diabetic cardiomyopathy, doxorubicin-induced cardiomyopathy, and septic cardiomyopathy. Numerous compounds have exerted potential therapeutic effects on cardiomyopathies by inhibiting ferroptosis. In this review, we summarize the core mechanism by which ferroptosis leads to the development of these cardiomyopathies. We emphasize the emerging types of therapeutic compounds that can inhibit ferroptosis and delineate their beneficial effects in treating cardiomyopathies. This review suggests that inhibiting ferroptosis pharmacologically may be a potential therapeutic strategy for cardiomyopathy treatment.

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“…Its intestinal absorption mechanism in rats was studied ( Zhang et al, 2012 ), when the complex was loaded into poly L-lactic acid scaffolds, the accumulated release percentage in vitro reached approximately 80% in 5 days ( Zhang et al, 2009b ). By using the dropping method, the inclusion complex of icariin with β -cyclodextrin was prepared, and the water solubility of icariin was increased only from 17 to 36 times though complexation ( Jin et al, 2012 ; Cui et al, 2013 ). Complexation of HP- β -cyclodextrin with icariin by stirring can only increase icariin’s water solubility about 4.3 times ( Wang et al, 2013b ).…”

Section: Introductionmentioning

confidence: 99%

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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Effect of β-cyclodextrin complexation on solubility and enzymatic hydrolysis rate of icariin

Cited by 14 publications

References 21 publications

Simple and novel icariin-loaded pro-glycymicelles as a functional food: physicochemical characteristics, in vitro biological activities, and in vivo experimental hyperlipidemia prevention evaluations

Simple and novel icariin-loaded pro-glycymicelles as a functional food: physicochemical characteristics, in vitro biological activities, and in vivo experimental hyperlipidemia prevention evaluations

Targeting ferroptosis as a promising therapeutic strategy to treat cardiomyopathy

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

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