Formulation and evaluation of mucoadhesive buccal films based on chitosan/hydroxylpropyl methylcellulose and chitosan/pectin

PICCIRILLI, G.N.; SALOMON, C.J.; BARRERA, M.G.; FRATTINI, A.; LEONARDI, D.; TEJADA, G.; SORTINO, M.; LAMAS, M.C.

Rosario

Congreso; IV Reunión Internacional de Ciencias Farmacéuticas; 2016

Chitosan (CH) is a cationic polyelectrolyte in aqueous acidic media. Several polymers form matrices with CH, modifying its physicochemical properties, among them are hydroxypropyl methylcellulose (HPMC) and pectin (PC). HPMC is a non ionic polymer and PC is a linear complex anionic polysaccharide. The aim of this work was the development of buccal mucoadhesive films based on CH in combination with PC and HPMC loaded with miconazole nitrate (MN), as a model drug. The films were thoroughly characterized in term of mechanical properties; adhesiveness; swelling; and MN release. Interactions between polymers were analyzed by infrared spectroscopy and the MN crystallinity studied by diferential scaning calorimetry (DSC). Finally, in vitro antifungal activity against Candida cultures was investigated. CH solutions (3% w/v) in lactic acid (10% v/v) were dripped on PC or HPMC (3% w/v), at 80 ºC under magnetic stirring. MN (2% w/w) was solubilized in PEG 400 (1 mL) and added to the polymeric solutions. The mixtures were stirred (200 rpm, 2h), cast on Petri dishes and dried. The thickness of all formulations (0.22-0.67 mm), were adequate to avoid the discomfort. The adhesive properties of CH have not been modified when it was combined whit PC or HPMC. The IR spectra of films based on CH and PC indicated strong interactions between -NH3+ groups of CH and the -COO- groups of PC. DSC studies showed that MN loaded in films was in an amorphous state. Films in vitro antifungal activity loaded with MN was higher than MN (raw material) and also higher than unloaded CH film Neither, PC nor HPMC showed activity against Candida cultures.