Improvement of the surface hydrophilic properties of naproxen particles with addition of hydroxypropylmethyl cellulose and sodium dodecyl sulphate: In vitro and in vivo studies

[Display omitted] In this study, a new surface-modified naproxen was developed to enhance brain concentration in acute migraine treatment. Fast-dissolving naproxen granules were made by mixing hydroxypropylmethylcellulose (HPMC) sodium dodecyl sulphate (SDS) and sodium croscarmellose with micronized...

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Published in:International journal of pharmaceutics 2017-08, Vol.529 (1-2), p.381-390
Main Authors: García-Herrero, Víctor, Torrado, Carlos, García-Rodríguez, Juan José, López-Sánchez, Alicia, Torrado, Susana, Torrado-Santiago, Santiago
Format: Article
Language:English
Subjects:
Animals
Disintegrant
Dissolution rate
Female
Hydrophobic and Hydrophilic Interactions
Hydroxypropylmethylcellulose (HPMC)
Hypromellose Derivatives - chemistry
Intestinal Absorption
Mice
Naproxen
Naproxen - chemistry
Naproxen - pharmacokinetics
Oral bioavailabilty
Sodium Dodecyl Sulfate - chemistry
Solubility
Surfactant
X-Ray Diffraction
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Summary:[Display omitted] In this study, a new surface-modified naproxen was developed to enhance brain concentration in acute migraine treatment. Fast-dissolving naproxen granules were made by mixing hydroxypropylmethylcellulose (HPMC) sodium dodecyl sulphate (SDS) and sodium croscarmellose with micronized naproxen particles. The aim of this study was to evaluate the effect of adding proportions of SDS to the HPMC film caused changes in the polymer chains of the HPMC, producing a new hydrophilic HPMC-SDS structure. These formulations with different HPMC/SDS ratios were characterised using electron microscopy (SEM), powder X-ray diffraction (PXRD), and differential scanning calorimetry (DSC). SDS 10% (w/w) produced a highly hydrophilic HPMC-SDS structure on the surface of the naproxen microparticles. The fast dissolution granules (SF-10%) showed a significant improvement in the dissolution rate of naproxen. Pharmacokinetic studies were conducted with mice, showing an improvement of Cmax (1.38 and 1.41-fold) and AUC0-2h (30% and 10% higher) for plasma and brain samples compared to the reference naproxen suspension. The faster Tmax ratio for SF-10% may be related to increased hydration in the gastrointestinal environment, enabling the drug to permeate the gastrointestinal hydration layer more easily due to the presence of the hydrophilic HPMC-SDS structure in the formulation.
ISSN:0378-5173
1873-3476
DOI:10.1016/j.ijpharm.2017.07.028