Effect of Quaternary Ammonium Surfactant on Buccal Permeation of Budesonide Film Formulation: In Silico Docking Studies

Budesonide, an immunosuppressant glucocorticosteroid generally used to ameliorate chronic inflammation. Low bioavailability due to first pass metabolism decreases its therapeutic activity. The present study focuses on the formulation of a biodegradable buccoadhesive film for improvement of buccalpermeation. Transparent buccoadhesive films were prepared by incorporating budesonide in HPMC matrix with triethalonamine as a plasticizer and a number of surfactants. Absence of the characteristic drug melting peak at 252°C in Differential Scanning Calorimetry (DSC) thermogram study confirmed almost complete amorphization of the drug to a homogenous solid-solid mixture in the film. The characteristic Fourier-Transform Infrared Spectroscopy (FTIR) peak of pure drug showed the carbonyl stretching in between 1600–1900 cm−1 and C–O stretching at 1095 cm−1. Broadening of C–O stretching and masking of carbonyl stretching confirmed the drug polymer interaction. In vitro dissolution and ex-vivo buccal tissue permeation revealed upto 72% and more than 58% respectively using surfactants upto 6 hour of study. Enhanced buccal permeability and flux were found in presence of surfactant compared to its absence. New film formulation could be developed including surfactant for improved buccal permeation with expected increased bioavailability. The in silico study confirmed about a stable interaction between drug and polymer (−3.1 kcal/mol)

Effect of Quaternary Ammonium Surfactant on Buccal Permeation of Budesonide Film Formulation: In Silico Docking Studies

1259-1266Budesonide, an immunosuppressant glucocorticosteroid generally used to ameliorate chronic inflammation. Low bioavailability due to first pass metabolism decreases its therapeutic activity. The present study focuses on the formulation of a biodegradable buccoadhesive film for improvement of buccalpermeation. Transparent buccoadhesive films were prepared by incorporating budesonide in HPMC matrix with triethalonamine as a plasticizer and a number of surfactants. Absence of the characteristic drug melting peak at 252C in Differential Scanning Calorimetry (DSC) thermogram study confirmed almost complete amorphization of the drug to a homogenous solid-solid mixture in the film. The characteristic Fourier-Transform Infrared Spectroscopy (FTIR) peak of pure drug showed the carbonyl stretching in between 1600–1900 cm−1 and C–O stretching at 1095 cm−1. Broadening of C–O stretching and masking of carbonyl stretching confirmed the drug polymer interaction. In vitro dissolution and ex-vivo buccal tissue permeation revealed upto 72% and more than 58% respectively using surfactants upto 6 hour of study. Enhanced buccal permeability and flux were found in presence of surfactant compared to its absence. New film formulation could be developed including surfactant for improved buccal permeation with expected increased bioavailability. The in silico study confirmed about a stable interaction between drug and polymer (−3.1 kcal/mol)