Preparation, Characterization, and In Vivo Evaluation of Amorphous Icaritin Nanoparticles Prepared by a Reactive Precipitation Technique Article Swipe
Cheng Tang
,
Kun Meng
,
Xiao‐Ming Chen
,
Hua Yao
,
Junqiong Kong
,
Fusu Li
,
Haiyan Yin
,
Mingji Jin
,
Hao Liang
,
Qipeng Yuan
·
YOU?
·
· 2021
· Open Access
·
· DOI: https://doi.org/10.3390/molecules26102913
YOU?
·
· 2021
· Open Access
·
· DOI: https://doi.org/10.3390/molecules26102913
Icaritin is a promising anti-hepatoma drug that is currently being tested in a phase-III clinical trial. A novel combination of amorphization and nanonization was used to enhance the oral bioavailability of icaritin. Amorphous icaritin nanoparticles (AINs) were prepared by a reactive precipitation technique (RPT). Fourier transform infrared spectrometry was used to investigate the mechanism underlying the formation of amorphous nanoparticles. AINs were characterized via scanning electron microscopy, X-ray powder diffraction, and differential scanning calorimetry. Our prepared AINs were also evaluated for their dissolution rates in vitro and oral bioavailability. The resultant nanosized AINs (64 nm) were amorphous and exhibited a higher dissolution rate than that derived from a previous oil-suspension formulation. Fourier transform infrared spectroscopy (FTIR) revealed that the C=O groups from the hydrophilic chain of polymers and the OH groups from icaritin formed hydrogen bonds that inhibited AIN crystallization and aggregation. Furthermore, an oral administration assay in beagle dogs showed that Cmax and AUClast of the dried AINs formulation were 3.3-fold and 4.5-fold higher than those of the oil-suspension preparation (p < 0.01), respectively. Our results demonstrate that the preparation of amorphous drug nanoparticles via our RPT may be a promising technique for improving the oral bioavailability of poorly water-soluble drugs.
Related Topics
Concepts
Bioavailability
Amorphous solid
Differential scanning calorimetry
Fourier transform infrared spectroscopy
Dissolution
Chemistry
Nanoparticle
Crystallization
Nuclear chemistry
Precipitation
Materials science
Chromatography
Chemical engineering
Pharmacology
Nanotechnology
Organic chemistry
Medicine
Physics
Thermodynamics
Meteorology
Engineering
Metadata
- Type
- article
- Language
- en
- Landing Page
- https://doi.org/10.3390/molecules26102913
- https://www.mdpi.com/1420-3049/26/10/2913/pdf?version=1620979854
- OA Status
- gold
- Cited By
- 11
- References
- 29
- Related Works
- 10
- OpenAlex ID
- https://openalex.org/W3160047216
All OpenAlex metadata
Raw OpenAlex JSON
- OpenAlex ID
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https://openalex.org/W3160047216Canonical identifier for this work in OpenAlex
- DOI
-
https://doi.org/10.3390/molecules26102913Digital Object Identifier
- Title
-
Preparation, Characterization, and In Vivo Evaluation of Amorphous Icaritin Nanoparticles Prepared by a Reactive Precipitation TechniqueWork title
- Type
-
articleOpenAlex work type
- Language
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enPrimary language
- Publication year
-
2021Year of publication
- Publication date
-
2021-05-14Full publication date if available
- Authors
-
Cheng Tang, Kun Meng, Xiao‐Ming Chen, Hua Yao, Junqiong Kong, Fusu Li, Haiyan Yin, Mingji Jin, Hao Liang, Qipeng YuanList of authors in order
- Landing page
-
https://doi.org/10.3390/molecules26102913Publisher landing page
- PDF URL
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https://www.mdpi.com/1420-3049/26/10/2913/pdf?version=1620979854Direct link to full text PDF
- Open access
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YesWhether a free full text is available
- OA status
-
goldOpen access status per OpenAlex
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https://www.mdpi.com/1420-3049/26/10/2913/pdf?version=1620979854Direct OA link when available
- Concepts
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Bioavailability, Amorphous solid, Differential scanning calorimetry, Fourier transform infrared spectroscopy, Dissolution, Chemistry, Nanoparticle, Crystallization, Nuclear chemistry, Precipitation, Materials science, Chromatography, Chemical engineering, Pharmacology, Nanotechnology, Organic chemistry, Medicine, Physics, Thermodynamics, Meteorology, EngineeringTop concepts (fields/topics) attached by OpenAlex
- Cited by
-
11Total citation count in OpenAlex
- Citations by year (recent)
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2025: 2, 2024: 2, 2023: 2, 2022: 4, 2021: 1Per-year citation counts (last 5 years)
- References (count)
-
29Number of works referenced by this work
- Related works (count)
-
10Other works algorithmically related by OpenAlex
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