Related Experiment Video
Updated: Jan 30, 2026
07:21
Twin-Screw Extrusion Process to Produce Renewable Fiberboards
Published on: January 27, 2021
7.1K
Fenofibrate Solid Dispersion Processed by Hot-Melt Extrusion: Elevated Bioavailability and Its Cell Transport
Ting Wen1, Boyi Niu1, Qiaoli Wu2
1School of Pharmaceutical Sciences, Sun Yat-Sen University, Guangzhou 510006, China.
Current Drug Delivery
|January 25, 2019
Summary
This study developed an amorphous solid dispersion of fenofibrate (FNB) using PVP VA64 via hot-melt extrusion. The new formulation significantly improved FNB
Area of Science:
- Pharmaceutical Technology
- Drug Delivery Systems
- Biopharmaceutics
Background:
- Fenofibrate (FNB) exhibits poor aqueous solubility, leading to low oral absorption and bioavailability.
- Effective treatment of hypertriglyceridemia and hypercholesterolemia is hindered by FNB's poor pharmacokinetic profile.
Purpose of the Study:
- To enhance the oral bioavailability of fenofibrate (FNB).
- To create an amorphous solid dispersion of FNB using PVP VA64 via hot-melt extrusion.
- To investigate the mechanism of improved drug absorption.
Main Methods:
- Amorphous solid dispersion preparation using hot-melt extrusion.
- Characterization via SEM, DSC, and XRD.
- In vitro evaluation using Caco-2 cells for cytotoxicity and permeation, and dissolution testing.
- In vivo pharmacokinetic study in beagle dogs.
Main Results:
- Hot-melt extrusion yielded an amorphous FNB solid dispersion with excellent carrier biocompatibility (PVP VA64).
- The amorphous solid dispersion demonstrated enhanced transmembrane transport and dissolution rates.
- Oral bioavailability of FNB solid dispersion was significantly increased by 2.45-fold compared to the commercial product.
Conclusions:
- PVP VA64 is a promising polymer for enhancing the bioavailability of poorly water-soluble drugs like FNB using hot-melt extrusion.
- This approach provides a foundation for developing effective solid dispersion formulations.
- Further mechanistic studies on enhanced penetration are warranted.
Related Concept Videos
02:54Molecular and Ionic Solids
20.0K
Crystalline solids are divided into four types: molecular, ionic, metallic, and covalent network based on the type of constituent units and their interparticle interactions.
Molecular Solids
Molecular crystalline solids, such as ice, sucrose (table sugar), and iodine, are solids that are composed of neutral molecules as their constituent units. These molecules are held together by weak intermolecular forces such as London dispersion forces, dipole-dipole interactions, or hydrogen bonds, which...
Molecular Solids
Molecular crystalline solids, such as ice, sucrose (table sugar), and iodine, are solids that are composed of neutral molecules as their constituent units. These molecules are held together by weak intermolecular forces such as London dispersion forces, dipole-dipole interactions, or hydrogen bonds, which...
20.0K
02:39Phase Transitions: Melting and Freezing
15.1K
Heating a crystalline solid increases the average energy of its atoms, molecules, or ions, and the solid gets hotter. At some point, the added energy becomes large enough to partially overcome the forces holding the molecules or ions of the solid in their fixed positions, and the solid begins the process of transitioning to the liquid state or melting. At this point, the temperature of the solid stops rising, despite the continual input of heat, and it remains constant until all of the solid is...
15.1K
02:18Network Covalent Solids
16.2K
Network covalent solids contain a three-dimensional network of covalently bonded atoms as found in the crystal structures of nonmetals like diamond, graphite, silicon, and some covalent compounds, such as silicon dioxide (sand) and silicon carbide (carborundum, the abrasive on sandpaper). Many minerals have networks of covalent bonds.
To break or to melt a covalent network solid, covalent bonds must be broken. Because covalent bonds are relatively strong, covalent network solids are typically...
To break or to melt a covalent network solid, covalent bonds must be broken. Because covalent bonds are relatively strong, covalent network solids are typically...
16.2K
03:12Freezing Point Depression and Boiling Point Elevation
40.0K
Boiling Point Elevation
The boiling point of a liquid is the temperature at which its vapor pressure is equal to ambient atmospheric pressure. Since the vapor pressure of a solution is lowered due to the presence of nonvolatile solutes, it stands to reason that the solution’s boiling point will subsequently be increased. Vapor pressure increases with temperature, and so a solution will require a higher temperature than will pure solvent to achieve any given vapor pressure, including one...
The boiling point of a liquid is the temperature at which its vapor pressure is equal to ambient atmospheric pressure. Since the vapor pressure of a solution is lowered due to the presence of nonvolatile solutes, it stands to reason that the solution’s boiling point will subsequently be increased. Vapor pressure increases with temperature, and so a solution will require a higher temperature than will pure solvent to achieve any given vapor pressure, including one...
40.0K
02:37Metallic Solids
20.6K
Metallic solids such as crystals of copper, aluminum, and iron are formed by metal atoms. The structure of metallic crystals is often described as a uniform distribution of atomic nuclei within a “sea” of delocalized electrons. The atoms within such a metallic solid are held together by a unique force known as metallic bonding that gives rise to many useful and varied bulk properties.
All metallic solids exhibit high thermal and electrical conductivity, metallic luster, and malleability....
All metallic solids exhibit high thermal and electrical conductivity, metallic luster, and malleability....
20.6K
02:34Comparing Intermolecular Forces: Melting Point, Boiling Point, and Miscibility
51.4K
Intermolecular forces are attractive forces that exist between molecules. They dictate several bulk properties, such as melting points, boiling points, and solubilities (miscibilities) of substances. Molar mass, molecular shape, and polarity affect the strength of different intermolecular forces, which influence the magnitude of physical properties across a family of molecules.
Temporary attractive forces like dispersion are present in all molecules, whether they are polar or nonpolar. They...
Temporary attractive forces like dispersion are present in all molecules, whether they are polar or nonpolar. They...
51.4K