ABSTRACT
The present study aimed to develop buccoadhesive film of glimepiride with unique combination of polymers and to investigate its effect(s) on physicomechanical parameters, drug-release, and permeation of films. Drug-polymer interaction was examined by FTIR and DSC analysis. Films were prepared by solvent casting technique and characterized for film strength (320 ± 8.5 g, 28.98 ± 2.00 mJ), buccoadhesive strength (28.8 ± 1.37 g, 3.04 ± 0.32 mJ), and tensile strength (260 ± 6.88 g, 18.00 ± 0.44 mJ) by new instrumental techniques. Increase in polymer concentration augmented zeta potential of polymeric matrix-mucin mixture and exhibited strong buccoadhesion (electrical theory). Buccoadhesion was also influenced by particle size (adsorption theory) and swelling (wetting theory). Erosion behavior of films was observed in swelling and SEM studies. Film GM4 exhibited 98 ± 2% in vitro drug release and 85 ± 8% ex vivo drug permeation in 12 h with controlled diffusion mechanism. Films were compatible with oral probiotic microorganisms. Stability studies revealed no significant (P < 0.05) variation in physicomechanical characteristics.
Subject(s)
Cellulose/administration & dosage , Cellulose/chemistry , Mouth Mucosa/metabolism , Sulfonylurea Compounds/administration & dosage , Sulfonylurea Compounds/chemistry , Adhesiveness , Administration, Buccal , Animals , Biological Availability , Diffusion , Drug Delivery Systems/methods , Goats , Particle Size , Permeability , Polymers/administration & dosage , Polymers/chemistry , Tensile StrengthABSTRACT
The aim of the present work was to develop and characterize mucoadhesive film of cellulose (methyl cellulose and hydroxy propyl methyl cellulose) and polymethacrylate (Eudragit RSPO) polymers for buccal delivery of carvedilol. Drug and polymers were found to be compatible as revealed by FTIR and DSC analysis. Mucoadhesive films were prepared by solvent casting technique. Swelling studies up to 4h did not show erosion of film, which was further confirmed by SEM analysis. New, simple and precise instrumental methods were established for the evaluation of mucoadhesive strength (33.8 ± 0.37-38.4 ± 0.24 g) and film strength (331.2 ± 0.73-369.0 ± 1.00 g) of developed films. Mucoadhesive film F5 showed 88 ± 1.15% in vitro drug release and 80 ± 2.30% ex vivo drug permeation through goat buccal mucosa in 12h. Drug release and permeation followed Higuchi's model and mechanism was found to be Fickian type diffusion controlled.
