Inulin as carriers for renal targeting delivery of ferulic acid

Abstract

Inulin (IN), as a classic diagnostic for determination of glomerular filtration rate, reached high concentration in kidney. Introducing drug into IN derivatives may be a new method to target kidney for drug delivery. To test the hypothesis, ferulic acid (FeA) was conjugated into IN by ester bond and amide bond (ethylenediamine as spacer), respectively, and the two FeA-IN conjugations, inulin ferulate (IN-FeA) and inulin ethylenediamine ferulate (IN-EDA-FeA) were obtained. NMR spectrum was involved to characterize the conjugations. The FeA in vitro release profiles were tested in mice plasma and renal homogenate. Finally, the biodistribution test was performed to evaluate their renal-targeting ability. Both IN-FeA and IN-EDA-FeA showed a higher release rate of FeA in renal homogenate than in mouse plasma suggesting the conjugates are relatively stable in plasma and more likely FeA release in kidney. The renal area under the curve (AUC) for IN-FeA and IN-EDA-FeA were 539.6 ± 107.9 and 558.5 ± 131.6 μg h/mL, respectively, which were 4.47 and 4.62 times of 120.8 ± 18.1 μg h/mL for free FeA. Meanwhile, significant smaller FeA accumulation in other organs was observed. These data indicated that IN-FeA and IN-EDA-FeA effectively targeted kidney for FeA delivery.

Keywords: Drug delivery; Ferulic acid; Inulin; Kidney targeting; Polysaccharide.