OBJECTIVES: The aim of this study was to prepare diclofenac/hydroxypropylmethylcellulose (HPMC) and diclofenac-loaded nanoparticles/HPMC films as potential systems for ocular delivery. METHODS: Two different concentration of the polymer were used: 1.5 and 2.0% w/v. Chitosan-hyaluronic acid nanoparticles were prepared by the ionotropic gelation technique. Nanoparticles were characterized by transmission electron microscopy, dynamic light scattering, drug encapsulation efficiency and rheological studies. In-vitro drug studies and corneal penetration release studies were carried out. Drug release mechanism was finally evaluated by fitting the Ritger and Peppas equation to data. In addition corneal hydration level was calculated to determine whether films could damage the corneas. KEY FINDINGS: Diclofenac HPMC films presented a faster drug release and a higher drug penetration than nanoparticles; on the contrary nanoparticles containing films were able to give a more sustained release of the drug and thus a slower diclofenac permeation through the cornea than HPMC films. CONCLUSIONS: Nanoparticles loaded with diclofenac sodium in HPMC films may be a valuable alternative for the treatment of ocular inflammatory diseases, since these formulations offer the benefit of sustained releasing directly to the site of action.
OBJECTIVES: The aim of this study was to prepare diclofenac/hydroxypropylmethylcellulose (HPMC) and diclofenac-loaded nanoparticles/HPMC films as potential systems for ocular delivery. METHODS: Two different concentration of the polymer were used: 1.5 and 2.0% w/v. Chitosan-hyaluronic acid nanoparticles were prepared by the ionotropic gelation technique. Nanoparticles were characterized by transmission electron microscopy, dynamic light scattering, drug encapsulation efficiency and rheological studies. In-vitro drug studies and corneal penetration release studies were carried out. Drug release mechanism was finally evaluated by fitting the Ritger and Peppas equation to data. In addition corneal hydration level was calculated to determine whether films could damage the corneas. KEY FINDINGS:DiclofenacHPMC films presented a faster drug release and a higher drug penetration than nanoparticles; on the contrary nanoparticles containing films were able to give a more sustained release of the drug and thus a slower diclofenac permeation through the cornea than HPMC films. CONCLUSIONS: Nanoparticles loaded with diclofenac sodium in HPMC films may be a valuable alternative for the treatment of ocular inflammatory diseases, since these formulations offer the benefit of sustained releasing directly to the site of action.
Authors: Ines Castangia; Maria Letizia Manca; Pietro Matricardi; Ana Catalán-Latorre; Amparo Nácher; Octavio Diez-Sales; Xavier Fernàndez-Busquets; Anna Maria Fadda; Maria Manconi Journal: J Mater Sci Mater Med Date: 2015-02-26 Impact factor: 3.896