Uricase from Bacillus fastidious loaded in alkaline enzymosomes: Enhanced biochemical and pharmacological characteristics in hypouricemic rats
| Autor: | Xiaoling Li, Huafeng Yin, Huarong Xiong, Jingqing Zhang, Yongzhen Teng, Dan He, Liangke Zhang, Jianyong Wu, Qunyou Tan, Chunjing Zhao, Na Wang |
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| Rok vydání: | 2012 |
| Předmět: |
Male
Fastidious organism Time Factors Urate Oxidase Pharmaceutical Science Bacillus Hyperuricemia Pharmacology Biology Rats Sprague-Dawley chemistry.chemical_compound medicine Animals Humans Liposome Half-life Urate oxidase General Medicine Hydrogen-Ion Concentration medicine.disease In vitro Rats Uric Acid Gout Disease Models Animal chemistry Biochemistry Injections Intravenous Liposomes Uric acid Rabbits Half-Life Biotechnology |
| Zdroj: | European Journal of Pharmaceutics and Biopharmaceutics. 82:43-48 |
| ISSN: | 0939-6411 |
| DOI: | 10.1016/j.ejpb.2012.06.002 |
| Popis: | 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 (t(1/2)) compared with free UBF, respectively. Further, it took only 4.5h (or 1.1h) for ESUBFs to lower the plasma uric acid concentration from a high level to the normal level of rat (or human beings), compared with 7.6h (or 5.4h) for free UBF. Our results showed that ESUBFs could efficiently deliver UBF and favorably modify its biochemical and pharmacological characteristics by increasing the AUC, t(1/2), and catalytic activity. Therefore, ESUBFs might be a preferred alternative to cure hyperuricemia and gout. |
| Databáze: | OpenAIRE |
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