FORMULATION AND DEVELOPMENT OF CELECOXIB OILY EYE DROPS
Author (s): Sanyasi Swain1*, Ajit Kumar Acharya2
Abstract: Steroids are used in the treatment of allergic ocular disorders, corneal burns, lacrimal tract inflammation, and other ocular inflammations but their use is limited by their tendency to increase intraocular pressure and to cause cataract upon chronic administration. Steroids also exacerbate ocular infections and diminish corneal/stromal wound healing. Non steroidal anti-inflammatory drugs (NSAIDs) like indomethacin, flurbiprofen, ketorolac, and diclofenac have been found to be viable alternatives to steroids in treating ocular inflammation. Celecoxib is a non-steroidal anti-inflammatory drug (NSAIDS), acts by inhibition of prostaglandins, by inhibiting the activity of the enzyme cyclooxygenase-2 (COX-2). The most convenient way of delivering drug to the eye is topical application of an aqueous solution. Drug from the aqueous solution partitions through the corneal epithelium, stroma, and endothelium into the aqueous humor. One principle demerit of topically applied aqueous drug solution is the loss of drug due to drainage which results in lower ocular availability of drug and a therapeutic effect of shorter duration. One way of overcoming the problem is to apply the drug in the form of an oily solution. Vegetable oils like olive, castor, and sesame oil are used as vehicles for oil-based drops. Considering the formulation factors as discussed, it can be concluded that celecoxib 0.5% (w/v) solution in sesame oil, being below the saturation level; containing benzyl alcohol (0.5%) could be the better choice for formulation.
Keywords: Celecoxib, sesame oil, benzyl alcohol, ocular inflammations