title: New Nanometric Solid Dispersions of Glibenclamide in Neusilin(®) UFL2.
abstract: To improve the poor water solubility and dissolution rate of the oral hypoglycemic drug glibenclamide, it was molecularly dispersed in Neusilin(®) UFL2, an amorphous synthetic form of magnesium aluminometasilicate, at different proportions; the physicochemical and biopharmaceutical properties, as well as the stability of the four different batches recovered were characterised, and it was determined that complete dispersion of glibenclamide in the amorphous polymer was obtained at the drug to Neusilin ratio of 1 to 2.5. Completely amorphous dispersion was proven by Thermal Analysis and X-Ray Powder Diffractometry. Very small particles were obtained, ranging from approximately 200 to 400 nm. The amorphous batches were physically and chemically stable for the entire duration of experiments. The physicochemical properties of the four batches were compared to those of the starting materials and physical mixtures of Neusilin(®) UFL2 and glibenclamide, the latter showing the typical behaviour of simple mixes, i.e., the additivity of properties of single components. The dissolution studies of the four solid dispersions revealed a very high dissolution rate of the completely amorphous batches (Batches 3 and 4), behaviour that was ascribed to their high Intrinsic dissolution rate due to the amorphous characteristics of the solid dispersions, to their very small particle size, and to the presence of polysorbate 80 that improved solid wettability. The technique under investigation thus proved effective for recovering stable amorphous dispersions of very small particle sizes.
authors.affiliation: School of Pharmacy, University of Camerino, Via S. Agostino, 1, 62032, Camerino, Italy.
authors.forename: Roberta
authors.initials: R
authors.lastname: Censi
authors.affiliation: School of Pharmacy, University of Camerino, Via S. Agostino, 1, 62032, Camerino, Italy.
authors.forename: Maria Rosa
authors.initials: MR
authors.lastname: Gigliobianco
authors.affiliation: School of Pharmacy, University of Camerino, Via S. Agostino, 1, 62032, Camerino, Italy.
authors.forename: Alessandra
authors.initials: A
authors.lastname: Dubbini
authors.affiliation: Faculty of Pharmacy, University of Medicine, Tirane, Albania.
authors.forename: Ladjan
authors.initials: L
authors.lastname: Malaj
authors.affiliation: School of Pharmacy, University of Camerino, Via S. Agostino, 1, 62032, Camerino, Italy. piera.dimartino@unicam.it.
authors.forename: Piera
authors.initials: P
authors.lastname: Di Martino
mesh_terms: D017607:Aluminum Compounds / Q000737:chemistry*; D002626:Chemistry, Pharmaceutical / Q000379:methods; D004355:Drug Stability; D005905:Glyburide / Q000737:chemistry*; D017616:Magnesium Compounds / Q000737:chemistry*; D053758:Nanoparticles / Q000737:chemistry*; D010316:Particle Size; D011136:Polysorbates / Q000737:chemistry; D011208:Powders / Q000737:chemistry; D017640:Silicates / Q000737:chemistry*; D012995:Solubility; D017155:Wettability; D014965:X-Rays
chemical_list: D017607:Aluminum Compounds; D017616:Magnesium Compounds; D011136:Polysorbates; D011208:Powders; D017640:Silicates; C033065:aluminum magnesium silicate; D005905:Glyburide
keywords: Neusilin® UFL2; dissolution; glibenclamide; particle size reduction; solid dispersions