Bioavailability Improvement Strategies for Icariin and Its Derivates: A Review
Abstract
:1. Introduction
2. Icariin and Its Derivates
2.1. Extraction and Preparation
2.2. Medicinal Properties
3. Bioavailability Improvements
3.1. Pharmaceutical Technologies
3.1.1. Complex Formation with Phospholipids
3.1.2. Complex Formation with Cyclodextrins
3.2. Nanotechnologies
3.2.1. Formation of Micelles
3.2.2. Nanocarriers
3.2.3. Nanogels
3.2.4. Nanocrystals
3.2.5. Microspheres
3.2.6. Extracellular Vesicles
3.2.7. Solid Lipid Nanoparticles
3.3. Structural Transformation
3.4. Absorption Enhancement
Colon-Specific Drug Delivery
4. Conclusions and Future Prospects
Author Contributions
Funding
Institutional Review Board Statement
Informed Consent Statement
Data Availability Statement
Conflicts of Interest
References
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Flavonol | Technique | Preparation Method | Carrier | Efficiency Improvement | Reference |
---|---|---|---|---|---|
Icariin | Complex formation | Lyophilization | β-Cyclodextrin | Cumulative drug release: 62% | [72] |
Complex formation | Lyophilization | β-Cyclodextrin | Solubility (water, 25 °C): 1.68-fold Absorption rate: 2.32-fold Permeability rate: 3.46-fold | [67] | |
Complex formation | Saturated solution method | β-Cyclodextrin | Solubility (water, 37 °C): 36-fold | [69] | |
Microspheres | Emulsion and coagulation | Gelatin and hyaluronic acid | Controlled release | [93] | |
Nanocarriers | Mixing and centrifuging | Fetal bovine serum exosomes | Cell proliferation significantly increased (p < 0.001) | [52] | |
Micelle | Mixing and vacuum-drying | PEG-PLLA/PDLA-PNIPAM polymers | Bioavailability: 5-fold | [88] | |
Solid modification | Heating | - | Solubility (water, 25 °C): 1.5-fold | [102] | |
Hydrogel formation | Photopolymerization | Hyaluronic acid | Controlled release | [92] | |
Hydrogel formation | Reverse microemulsion method | Span 80 and Tween 80 | - | [91] | |
Solid lipid nanoparticles | High temperature melt-cool solidification method | Liposomal vesicles | Bioavailability: 4-fold | [99] | |
Absorption enhancer | Mixing | Snailase | Bioavailability: 1.5-fold | [104] | |
Icariside II and icariin mixture | Complex formation | Wet media milling | Soybean phospholipids | ICA: Dissolution: 1.39-fold (2 h) Bioavailability: 2.38-fold ICS: Dissolution: 1.24-fold (2 h) Bioavailability: 6.57-fold | [65] |
Icariside II | Complex formation | Reduction vaporization | Phospholipid | Bioavailability: 3.45-fold | [60] |
Complex formation and micelles | Solvent evaporation | Phospholipid and vitamin E TPGS 1000 | Bioavailability: 5.33-fold | [63] | |
Micelles | Thin film hydration | DDAB and TPGS with hyaluronic acid | Controlled release | [84] | |
Micelles | Solvent evaporation | Solutol® HS15 and Pluronic F127 | Solubility (water, temperature not mentioned) 900-fold Bioavailability: 3.17-fold | [83] | |
Nanocarriers | Incubation and sonification | Bovine milk as extracellular vesicles | - | [96] | |
Icaritin | Nanocrystal | Antisolvent-precipitation | Hydroxypropyl methylcellulose as stabilizer | Bioavailability: 2.01-fold | [54] |
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Szabó, R.; Rácz, C.P.; Dulf, F.V. Bioavailability Improvement Strategies for Icariin and Its Derivates: A Review. Int. J. Mol. Sci. 2022, 23, 7519. https://doi.org/10.3390/ijms23147519
Szabó R, Rácz CP, Dulf FV. Bioavailability Improvement Strategies for Icariin and Its Derivates: A Review. International Journal of Molecular Sciences. 2022; 23(14):7519. https://doi.org/10.3390/ijms23147519
Chicago/Turabian StyleSzabó, Róbert, Csaba Pál Rácz, and Francisc Vasile Dulf. 2022. "Bioavailability Improvement Strategies for Icariin and Its Derivates: A Review" International Journal of Molecular Sciences 23, no. 14: 7519. https://doi.org/10.3390/ijms23147519