Development of buccal Mucoadhesive films containing Triamcinolone Acetonide from Durian-fruit hull gel

Abstract

Polysaccharide gel (PG) was extracted from dried durian-fruit hull. Calcium gluconate was a suitable crosslinking agent for PG. Bilayered buccal mucoadhesive films with and without triamcinolone acetonide (TAA) were formulated, Casting preparation of the bilayered films consisted of a mucoadhesive layer prepared by using 5 % PG as a film-forming agent and a backing layer prepared by using 5 % w/v ethylcellulose. Plasticizers in the mucoadhesive layer include 30 % w/w glycerin, 30 % w/w sorbitol, and 1% w/w polyethylene glycol 6000 based on the PG weight in preparations which provided the greatest tensile strength, % elongation and mucoadhesion force. Eudragit® RL 100, Eudragit® RS 100, Eudragit® NE 30D, or Kollicoat® SR 30 D was added to retard the dissolution of mycoadhesive layer; only 12.5 % w/w Eudragit® RL 100 and Kollicoat® SR 30 D provided continuous films. Eudragit® RL 100 was chosen because the films formed had the greatest tensile strength, % elongation, work of failure, Young’s modulus, force of mucoadhesion, and work of adhesion. TAA significantly reduced both force and work of mucoadhesion (p<0.05). The loss of TAA in PG films were less than 10 % when stored at 40 °C, 75% RH for 3 months. The release of TAA from PG films followed nonFickian mechanism and was completed within 3 hours. Clinical test of buccal mucoadhesive film products were also performed. Seventy-two subjects showing a sign of aphthous stomatitis were randomly and equally grouped into the following 4 groups: untreated (control), PG film base treated, PG films with TAA treated, and Kenalog® in orabase treated groups. All preparations showed comparable residence time on the subjects’ buccal mucosa. The curing rate of all treated subjects were significantly faster than those untreated (p<0.05). The time periods of ulcer disappearance were significantly reduced (p<0.05) in the treated group using PG film base.