Entrapment of ketorolac tromethamine in polymeric vehicle for controlled drug delivery

• Published in: Indian journal of pharmaceutical sciences Vol. 71; no. 6; pp. 687 - 691
• Main Authors: Paliwal, S K, Chauhan, Rajani, Sharma, Veena, Majumdar, D K, Paliwal, S
• Format: Journal Article
• Language: English
• Published: India Medknow Publications and Media Pvt. Ltd 01-11-2009; Medknow Publications & Media Pvt. Ltd; Medknow Publications
• Subjects: Drug delivery systems; Drugs; Health aspects; Ketorolac; Nonsteroidal anti-inflammatory drugs; Pharmaceuticals; Pharmacology; Polymers; Short Communication; Vehicles; India; controlled drug delivery; polymeric vehicle; goat eye; ketorolac tromethamine; Corneal permeation
• ISSN: 0250-474X; 1998-3743
• DOI: 10.4103/0250-474X.59555

The most common method for applying a drug in to the eye is to formulate the drug in the form of an eye drop, but this method is not considered ideal for ocular delivery of drug because of poor bioavailability arising from precorneal loss processes, this loss of drug from the precorneal area is a net effect of drainage, tear secretion and noncorneal absorption. Following the above lead we tried to improve the ocular bioavailability by increasing the corneal contact time and the feasible way was to formulate a drug with mucoadhesive/viscosity imparting agents. The adhesive strength of various polymers on corneal surface was studied with the help of self modified Franz diffusion cell and freshly excised goat/bovine cornea. The polymers hydroxypropylmethylcellulose, carboxymethylcellulose sodium, Eudragit type E/RL/RS, Carbopol ETD 2020 and Carbopol 934 National Formulary were formulated with drug, ketorolac tromethamine. The adhesive strength of polymers on corneal surface and permeation characteristics of drug through cornea were investigated by using above said formulations. Eudragit type E/RL/RS did not show any improvement in mucoadhesion, but the formulations containing Carbopol ETD 2020 and Carbopol 934 national formulary showed good mucoadhesion on corneal surface in the concentration as low as 0.75%. The mucoadhesive strength was also evaluated using the combination of Carbopol acrylates/C 10-30 alkylacrylate with allylpentaerithrital and preservative benzalkonium chloride, which also resulted in good mucoadhesion with improved corneal permeation. Observations made in this study indicate the potentiality of the ophthalmic formulations containing mucoadhesive/viscosity imparting agents.