Effect of Transcutol and Stearylamine on Ibuprofen Hydrophilic Gel for Transdermal Delivery

Abstract

Transdermal drug delivery system (TDDS) shows promising results when compared with oral drug delivery system mainly by eliminating the first pass metabolism and by improving the bioavailability of drug. Hydrophilic gels are networks of polymer chains that are sometimes found as colloidal gels in which water is the dispersion medium. Ibuprofen, nonsteroidal anti-inflammatory drug used to relieve pain, reduces fever and anti-inflammation. The purpose of present research is to demonstrate the influence of various enhancers (transcutol and stearylamine) in various concentrations on percutaneous permeation of ibuprofen hydrophilic gel from HPMC K4M & HPMC K100M gel formulation. Gelling agents at various concentrations were preliminary screened for gel consistency. The control and the prepared gels were evaluated for clarity, homogeneity, spreadability, extrudability, drug content, invitro diffusion, ex-vivo permeation, skin irritation, anti-inflammatory activity and stability studies. All formulations have shown better physicochemical properties. Ex-vivo skin permeation studies reveals that the (IBU29) formulated using HPMC K4M 6%, transcutol 40% and stearylamine 4% as permeation enhancers has shown maximum drug release of 86.4 % for 24hrs. Permeability parameters like flux were found to be 1940.68±0.06µg/cm²/hr, permeability coefficient was found 31 ×10-3 cm/hr and Q24 was found to be 5240.82±0.06µg/cm² and enhancement ratio of 13.06 over pure drug. Skin irritation studies showed irritation potential of “0” score thus providing to be non-irritant. The anti-inflammation studies were performed with inflammation induced by carrageenan 1% w/v solution. Optimized formulation (IBU29) showed highest reduction of inflammation comparable to marketed preparation BRUGESIC GEL®. The formulations were stable at room temperature for 1 month.Key words: Transdermal gel, Ibuprofen, HPMC K4M, HPMC K100M, Penetration- enhancer..