Binding of nonsteroidal anti-inflammatory drugs to DPPC: Structure and thermodynamic aspects

• Type: Article in International Scientific Journal
• Date: 2008

Authors

Marlene Lucio (Author) FFUP; Frank Bringezu (Author) Other; Salette Reis (Author) FFUP; Jose L F C Lima (Author) FFUP; Gerald Brezesinski (Author) Other

Journal

Title: Langmuir

Vol. 24 No. 16

Pages: 4132-4139

ISSN: 0743-7463

Publisher: American Chemical Society

Indexing

ISI Web of Knowledge - 59 Citations

Scopus - 69 Citations

Pubmed / Medline

Scientific classification

FOS: Engineering and technology > Materials engineering

CORDIS: Health sciences

Other information

Authenticus ID: P-004-05J

DOI: 10.1021/la703584s

Resumo (PT): The effect of nonsteroidal anti-inflammatory drugs (NSAIDs) on the phase transition and phase properties of 1,2-dipalmitoylphosphatidylcholine (DPPC) has been investigated in both 2D (monolayers at the air/water interface) and 3D (multilayers in lipid/water dispersions) model systems. The 2D membrane models have been characterized by means of pressure−area isotherms and grazing incidence X-ray diffraction (GIXD) measurements. Differential scanning calorimetry (DSC) and simultaneous small- and wide-angle X-ray diffraction have been applied to lipid aqueous dispersions. All NSAIDs studied altered the main transition temperature of the gel to liquid-crystalline phase transition, with the arylacetic acid derivatives (acemetacin and indomethacin) showing the largest effects. A comparison of the results reveals distinct structural features of the membrane models after interaction with the NSAID. All drugs induced perturbations in the lipid liquid-crystalline phase, suggesting a major change in the hydration behavior of DPPC. Again, the largest effects on the structural parameters are found for the arylacetic acid derivatives. The results obtained in the different model systems give indications of the role of the membrane/NSAID interactions that might also be important for NSAID gastric injury. <br> <br> <a target="_blank" href="http://pubs.acs.org/doi/abs/10.1021/la703584s"> Texto integral </a> <br> <br>

Abstract (EN): The effect of nonsteroidal anti-inflammatory drugs (NSAIDs) on the phase transition and phase properties of 1.2-dipalmitoylphosphatidylcholine (DPPC) has been investigated in both 2D (monolayers at the air/water interface) and 3D (multilayers in lipid/water dispersions) model systems. The 2D membrane models have been characterized by means of pressure-area isotherms and grazing incidence X-ray diffraction (GIXD) measurements. Differential scanning calorimetry (DSC) and simultaneous small- and wide-angle X-ray diffraction have been applied to lipid aqueous dispersions. All NSAIDs studied altered the main transition temperature of the gel to liquid-crystalline phase transition. with the arylacetic acid derivatives (acemetacin and indomethacin) showing the largest effects. A comparison of the results reveals distinct structural features of the membrane models after interaction with the NSAID. All drugs induced perturbations in the lipid liquid-crystalline phase, suggesting a major change in the hydration behavior of DPPC. Again, the largest effects on the structural parameters are found for the arylacetic acid derivatives. The results obtained in the different model systems give indications of the role of the membrane/NSAID interactions that might also be important for NSAID gastric injury.

Language: English

Type (Professor's evaluation): Scientific

No. of pages: 8