Improved in vivo performance and immunomodulatory effect of novel Omega-3 fatty acid based Tacrolimus nanostructured lipid carrier

Abstract

The objective of this study was to enhance in vivo performance of Tacrolimus (TL) by means of its novel nanostructured lipid carrier (NLC) incorporated with characteristic lipids and surfactants. Solid lipid employed was Compritol 888ATO, liquid lipid applied was omega-3 fatty acid which constitutes exorbitant characteristic immunomodulatory property. In addition, the surfactant used was Solutol HS15. The NLC of TL were formulated, characterized and investigated for their enhanced lymphatic and immunosuppressive distinction. The in vitro lipolysis studies disclosed significantly high solubilisation (***p < 0.001) of OMEGA-NLC in aqueous phase (70.1%) in contrast to TL suspension (1.6%). The lymphatic distribution of OMEGA-NLC was noticeably enhanced by 80.84 and 19.58 folds in comparison to TL suspension and N-NLC (without omega-3 fatty acid), respectively. Furthermore, OMEGA-NLC demonstrated significantly minimized (***p < 0.001) interleukin 2 (IL-2) release of 66.5 pg/ml in contrast to TL suspension (520 pg/ml) and N-NLC (408 pg/ml) stipulating enhanced immunosuppressive action by incorporated omega-3 fatty acid. The findings of the study substantiated that omega-3 fatty acid based NLC could strikingly enhance immunosuppressive therapeutic attributes and it is a potential alternative that can be utilized successfully in immunosuppressive drug therapy regimen with minimized toxicity concerns.