토끼의 각막 추출액 중 메치오닌엔케팔린 및 [D-알라$^2$-메치오닌엔케팔린아미드의 분해 및 안정화

Degradation and Stabilization of Methionine Enkephalin and $[D-Ala^2]-methionine$ Enkephalinamide in the Corneal Extracts of Rabbits

In order to study systemic peptide delivery through the ocular route, the stabilities of methionine enkephalin (Met-Enk) and $[D-ala^2]-methionine$ enkephalinamide (YAGFM) in the corneal extracts of rabbits were investigated using reversed phase HPLC. Met-Enk was found to be hydrolyzed most rapidly in the corneal epithelium, but YAGFM was relatively stable. Aminopeptidases appeared to contribute over 60% to the degradation of Met-Enk and the degradation rate of Met-Enk followed the first order kinetics. The half-lives of Met-Enk in the extracts of the corneal epithelium and endothelium were 36 and 673 min, respectively. From the effects of enzyme inhibitors, it was found that the application of the mixture of amastatin, thimerosal and EDTA was very useful for the inhibition of peptide degradation.