Preparation, characterisation and photosensitivity studies of solid dispersions of diflunisal and Eudragit RS100 and RL100.
Solid dispersions of diflunisal (DIF) with Eudragit RS100 (RS) and RL100 (RL) with different drug-to-polymer ratios were prepared by a solvent method (coevaporates) and were characterised in the solid state in comparison with the corresponding physical mixtures. The work was aimed at characterising the interactions occurring between DIF and RS or RL polymers, along with their influence on the in-vitro drug-dissolution pattern. The findings suggest that the drug did not change its crystalline form within the polymer network. Drug dispersion in the polymer matrix strongly influences its dissolution rate, which appears slower and more gradual while increasing the polymer ratios. Moreover, DIF is known to be a photosensitive compound, and its photoproduct has been found to be a toxic agent. This can be evidenced by testing red blood cell membranes for their resistance to the osmotic shock induced by UVA irradiation in the presence of DIF. The presence of some DIF/RS coevaporates was shown to reduce significantly the drug photosensitization process towards cell membranes. This suggests the possibility of combining the design of a drug delivery system with a photoprotective strategy.
Pignatello
R
R
Dipartimento di Scienze Farmaceutiche, Università di Catania, Viale A. Doria, 6-I-95125, Catania, Italy.
Ferro
M
M
De Guidi
G
G
Salemi
G
G
Vandelli
M A
MA
Guccione
S
S
Geppi
M
M
Forte
C
C
Puglisi
G
G
D000180:Acrylic Resins / Q000737:chemistry*; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D002152:Calorimetry, Differential Scanning; D004061:Diflunisal / Q000737:chemistry* / Q000493:pharmacokinetics / Q000494:pharmacology; D004910:Erythrocyte Membrane / Q000187:drug effects / Q000378:metabolism / Q000528:radiation effects; D006801:Humans; D009682:Magnetic Resonance Spectroscopy; D011108:Polymers / Q000737:chemistry; D012997:Solvents / Q000737:chemistry; D017550:Spectroscopy, Fourier Transform Infrared; D014466:Ultraviolet Rays; D014961:X-Ray Diffraction
D000180:Acrylic Resins; D000894:Anti-Inflammatory Agents, Non-Steroidal; D011108:Polymers; D012997:Solvents; C050528:Eudragit RS; D004061:Diflunisal