FLURBIPROFEN OPHTHALMIC SOLUTIONS TARGETING THE POSTERIOR SEGMENT OF EYE: AN EX-VIVO STUDY AND A NOVEL PRODRUG APPROACH ON EXCISED GOAT CORNEA

Ugandar R. E.*, Dinesh Kumar Sharma, Kiran C. Nilugal and Nagashekhara Molugulu

ABSTRACT

The current research involves the study of enhancement of trans-corneal permeation Non- Steroidal Anti-Inflammatory Drug, Flurbiprofen via amino acid transporters through excised goat cornea. The prodrug approach by esterification of amino acids followed by conjugation of the amino acid esters with the drug through solvent evaporation technique has been adopted for the synthesis of the physical mixtures of esterified amino acids conjugated with Flurbiprofen. The physical mixtures obtained were characterized by several analytical techniques, purified and were used as active ingredients for preparing the test formulations of Flurbiprofen. In the study, three categories of conjugated physical mixtures of Flurbiprofen with three different amino acids such as L-Arginine, L-Tyrosine and L- valine were synthesized initially by esterification of the amino acids to get methyl and ethyl esters of the amino acids followed by conjugation with Flurbiprofen. The purified products were used as active ingredients for different test formulations of Flurbiprofen. The results obtained from the trans-corneal permeation studies on excised goat cornea during the ex-vivo studies by using a Franz diffusion cell were compared with those of the standard ophthalmic formulations of Flurbiprofen. All results revealed that the permeation of drugs with the amino acid transporters were found to be enhanced through excised goat cornea when compared with the results of the prepared standard formulation of Flurbiprofen.

Keywords: Flurbiprofen, pro-drug, permeation, ex-vivo, diffusion, & amino acid transporters.