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Fabricating Superhydrophobic Polymeric Materials for Biomedical Applications
Published on: August 28, 2015
Differences in the interaction between aryl propionic acid derivatives and poly(vinylpyrrolidone) K30: A
Zehadin Gashi1, Roberta Censi, Ledjan Malaj
1Department of Pharmacy, University of Tirana, Street of Dibra, Tirana, Albania.
Journal of Pharmaceutical Sciences
|August 1, 2009
Summary
Ibuprofen (IBP) strongly interacts with poly(vinylpyrrolidone) (PVP) K30, unlike other NSAIDs, due to its low molar volume and crystal lattice weakness. This interaction influences drug diffusion and amorphous phase stabilization within the polymer matrix.
Area of Science:
- Physical Chemistry
- Materials Science
- Pharmaceutical Sciences
Background:
- Aryl propionic acid derivatives, including ibuprofen (IBP), ketoprofen (KET), flurbiprofen (FLU), naproxen (NAP), and fenbufen (FEN), are commonly used non-steroidal anti-inflammatory drugs (NSAIDs).
- Poly(vinylpyrrolidone) (PVP) K30 is a widely used polymer excipient in pharmaceutical formulations, known for its ability to form solid dispersions with drugs.
Purpose of the Study:
- To investigate and explain the differential physical interactions between several aryl propionic acid derivatives and poly(vinylpyrrolidone) (PVP) K30.
- To elucidate the factors governing drug-polymer interactions, diffusion mechanisms, and the resulting changes in physical properties like glass transition temperature (T(g)).
Main Methods:
- X-ray powder diffractometry and (13)C-solid state Nuclear Magnetic Resonance (NMR) spectroscopy to assess drug-polymer interactions.
- Differential Scanning Calorimetry (DSC) using the Gordon-Taylor equation to study melt-processed drug-PVP mixtures.
- Molecular docking simulations to analyze intermolecular forces and binding energies.
- Solid-state kinetic studies to determine drug diffusion mechanisms.
Main Results:
- Ibuprofen (IBP) exhibited strong interaction with PVP K30, while ketoprofen (KET), flurbiprofen (FLU), naproxen (NAP), and fenbufen (FEN) showed progressively weaker interactions.
- Lower molar drug volumes were found to favor drug diffusion into PVP amorphous chains, increasing polymer free volume and decreasing mixture T(g).
- Molecular docking indicated that van der Waals forces and drug-PVP surface contact area significantly influence interaction strength.
- IBP's diffusion followed a three-dimensional mechanism, facilitated by its low molar volume and weak crystal lattice, promoting amorphous phase stabilization.
Conclusions:
- The physical interaction strength between aryl propionic acid derivatives and PVP K30 is drug-specific and influenced by molecular properties like molar volume and crystal lattice energy.
- Understanding these interactions is crucial for designing stable and effective pharmaceutical solid dispersions.
- IBP's unique interaction profile with PVP suggests potential advantages for its formulation in amorphous solid dispersions.
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