| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 2085292 | European Journal of Pharmaceutics and Biopharmaceutics | 2012 | 6 Pages |
The aim of this study was to assess the potential of a novel alkaline enzymosome to deliver uricase from Bacillus fastidious (UBF) and enhance its biochemical and pharmacological characteristics. The in vitro catalytic activity of the UBF loaded in the novel alkaline enzymosomes (ESUBFs) was almost 3.8 times that of free UBF at the optimum pH or 1.5 times that of free UBF at the physiological pH. Following intravenous (i.v.) administration (2000 mU/kg) in rats, ESUBFs provided significantly higher (22.5-fold) area under the plasma concentration (AUC) and longer (8.2-fold) circulation half-life (t1/2) compared with free UBF, respectively. Further, it took only 4.5 h (or 1.1 h) for ESUBFs to lower the plasma uric acid concentration from a high level to the normal level of rat (or human beings), compared with 7.6 h (or 5.4 h) for free UBF. Our results showed that ESUBFs could efficiently deliver UBF and favorably modify its biochemical and pharmacological characteristics by increasing the AUC, t1/2, and catalytic activity. Therefore, ESUBFs might be a preferred alternative to cure hyperuricemia and gout.
Graphical abstractAlkaline enzymosomes containing uricase from Bacillus fastidious: improved biochemical properties in vitro and pharmacological characteristics in vivo.Figure optionsDownload full-size imageDownload high-quality image (100 K)Download as PowerPoint slide
