Budesonide, a glucocorticosteroid is generally used to treat chronic inflammation and asthma. Hepatic first-pass metabolism and poor solubility are the major causes of its limited oral bioavailability. Present work was undertaken for the preparation of hydrogel film formulation with cyclodextrin complexation of budesonide containing quaternary surfactant for possible enhancement of mucosal permeation. FTIR study confirmed drug-polymer hydrogen bonding. Almost complete amorphization of the drug was pronounced by SEM, DSC and XRD studies. The film containing benzalkonium and hydroxypropyl beta-cyclodextrin exhibited in vitro dissolution and mucosal permeation to the highest extent of 87.2 and 95.8 % respectively in contrast to the others. Film formed hydrogel in aqueous mucin and enhanced the mucosal tissue residence time due to the mucoadhesive nature of the polymer. Acute inflammation in the rabbit eye was controlled within 3 h by applying the film in the cul-de-sac. The presence of cyclodextrin and quaternary surfactant brought about significantly improved drug release and mucosal permeation compared to their absence in the HPMC film. Hydrogel formed in aqueous mucin enhanced the mucosal residence time and controlled acute inflammation in the rabbit eye within 3 h after topical application.

Ocular drug delivery in hydrogel forming film form has several benefits over conventional dosage forms. Ophthalmic anti-inflammation study have been undertaken using topically applied aspirin in hydrogel film formulation. Hydroxypropyl methylcellulose (HPMC) matrix film formulation was prepared by solvent casting and evaporation technique by taking triethanolamine (TEA) as a plasticizer. Ex vivo corneal permeation as well as anti-inflammatory potential of aspirin was studied on carrageenan induced rabbit eye model. Moisture uptake was found to be in the range of 17.097 and 19.139 % for all the film formulations. Higher HPMC content in the film exhibited increased both the moisture uptake and content of swelling. Among the formulations the swelling order was found to be increasing according to the increasing amount of HPMC in the film. Presence of hydrogel matrix forming polymer sustained the drug release and corneal permeation for more than 6 h and controlled the process by diffusion mechanism. The signs of carrageenan induced acute inflammation have been inhibited completely just within 2 h of placing the film in the rabbit eye whilst the positive control continued showing redness and increased tear secretion. Aspirin ocular film formulation could be utilized for ocular anti-inflammation for an extended period of time with better patient compliance.