Diclofenac peptides

Diclofenac, a derivative of phenylacetic acid, is equipotent as an inhibitor of COX-1 and COX-2. In addition to prostaglandin inhibition a central analgesic action of diclofenac mediated by endogenous opioid peptides has been demonstrated. It can be administered orally, intramuscularly or intravenously, and is effective as a postoperative analgesic in a dose of 75-150 mg. The risks of adverse gastrointestinal effects is moderate and diclofenac does not appear to increase blood loss during or after surgery. 

Cohen-Avrahami et al. examined the feasibility of a system based on Hn meso-phase loaded with a skin penetration enhancer and sodium diclofenac (Na-DFC) [44]. They used a penetration enhancer (RALA, a 16 amino-acid long peptide) belonging to a synthetic family of CPEs, based on GALA, amphipathic peptides. These peptides contain an alanine-leucine-alanine repeating unit that exhibited improved membrane permeability [104]. 

M. Cohen-Avrahami, A. Aserin, N. Garti, Hn mesophase and peptide cell-penetrating enhancers for improved transdermal delivery of sodium diclofenac. Colloids Surf. B 77, 131-138 (2010)... 

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