| Abstrakt: |
Background: Inflammation has become the culmination point for several chronic diseaseslike skin diseases, asthma, neurological disorders, cancer, and cardiovascular disorders. MiniαA-crystallin peptide, identified from a highly conserved region of human lens protein αA-crystallin,is known to have a chaperone-like function; hence, it has generated interest in exploring theanti-inflammatory potential of the peptide. Objective: The objective of the study was to evaluate the anti-inflammatory potential of mini αAchaperones using in vitro, ex-vivo, and in vivo models. Methods: The peptide was tested for its phosphodiestarase4 B inhibition, anti-inflammatory andfree radical scavenging abilities in HaCaT cells. Carbopol gel formulations with varying concentrationsof mini αA-crystallin peptide and diclofenac sodium were prepared and optimized. Skinpermeation studies of prepared formulations were carried out on excised abdominal skin of Wistarrat using a vertical type diffusion cell. Carrageenan induced rat paw oedema model was used for determiningthe anti-inflammatory potential of the peptide in prepared gel formulation with or withoutdiclofenac sodium. Results: The peptide exhibited appreciable free radical scavenging and weak PDE4B inhibition.Gel formulation with 1% Tween-80, 1% carbopol, and 10% ethanol showed better permeation comparedto other formulations. The in vitro skin permeation studies revealed good improvement inpermeation characteristics of diclofenac and peptide from the gels. The peptide was retained withinthe skin tissue, which is an ideal requirement for the delivery of an anti-inflammatory topical formulation.In preclinical anti-inflammatory studies, gel formulation containing mini αA-peptide anddiclofenac sodium showed a significant decrease in paw volume compared to other combinationstested. Conclusion: The study revealed the additive effect in anti-inflammatory activity by combiningmini-αA peptide and diclofenac sodium which effectively reduced the inflammation. |
