Skin targeted delivery of rutin-phospholipid complex: Patch formulation, in vitro-in vivo evaluation

Abstract

Oral bioavailability of Rutin is very low due to solubility issues and first pass effects. Rutin-phospholipid complexes (RN-P)s offer improved physicochemical properties favorable for drug delivery via the skin. The present work aims to develop sustained release polymeric patch containing RN-Ps to treat inflammation. Patch prepared by solvent evaporation method using polymers (Eudragit RL 100, PVP K30) and plasticizer (PEG 400). Prepared patch were studied for film properties. SEM and TEM images were used to study surface morphology. FE-SEM images of the patch taken after drug release and skin permeation. Sustained anti-inflammatory effect was established in carrageenan induced paw edema model. A 7 (seven) days skin irritation test on rabbit was performed. Optimized formulation gave 85.12 % drug release and 31.0 % cumulative permeation in 24 hours studies. Skin penetration and accumulation were found higher with RN-P than pure rutin. FE-SEM images showed that RN-Ps retain their structure after 24 hours exposure to physiologic environment. The test formulation gave 91.4 % inhibition of inflammation at 24 hours as compared to 39.58 % for standard. Skin irritation test revealed that the patches are safe for skin application. We conclude that polymeric transdermal patch able to deliver RN-Ps for sustained therapeutic effect useful in treating acute and chronic inflammation.