| Epidemiologically speaking, it is estimated that 350 million people are infected with HBV and 170 million people worldwide are infected with HCV. For chronic viral hepatitis, interferon has been widely used, but it usually has a short half-life after intravenous or subcutaneous administration. Thus, it has become one of important tasks that to reconstitute interferon for prevention of rapid degradation and half-life. Albuferon is a novel, long-acting form of interferon alpha and has become one of important topics, but HSA-IFNα2b is a compound of poor liver-targeting for treating viral hepatitis.The purpose of this article is to enhance the liver-targeting ability of HSA-IFNα2b. We have prepared GHSA-IFNα2b.The protein concentration of GHSA-IFNα2b was 250μg/ml, and the sugar concentration of GHSA-IFNα2b solution was 14.4μg/ml.Consequently,the GHSA-IFNα2b could be calculated to be 24 galactose groups per HSA-IFNα2b.The purpose of this thesis is to evaluate the liver-targeting ability of 99Tcm-GHSA-IFNα2b.99Tcm-GHSA-IFNα2b was prepared by the reduction of Na99TcmO4 with SnCl2 and the radiolabeled compound was characterized by polyamide TLC, in which 20mmol/L PBS pH7.2:10%SDS:acetone(V:V:V)=3:1:1 was used as the developing agent. The effects of the amounts of SnCl2, GHSA-IFNα2b, and pH value on the labeling yield of 99Tcm-GHSA-IFNα2b were investigated. The experimental results proved that labeling yield of 99Tcm-GHSA-IFNα2b could be over 90% under the following labeling conditions: pH value was between 3.0 and 4.5, the amounts of GHSA-IFNα2b was over 0.3mg, the content of SnCl2 was between 3μg and 60μg, and the labeling reaction continued for 30min at 37℃.The biodistribution study was carried out in ICR mice. 0.2ml (0.286MBq) 99Tcm-GHSA-IFNα2b solution containing 2μg GHSA-IFNα2b was injected to each mouse through the tail vein. After injection, each group mice were decapitated at 5, 10, 15, 30, 60, and 120min, respectively. The interested organs were excised, weighed, and counted in the automatic gamma counter. The ID%/organ and ID%/g were calculated. The liver scan in rat of 99Tcm-GHSA-IFNα2b was also studied. Biodistribution in mice showed that the peak of liver uptake of 99Tcm-GHSA-IFNα2b was reached at 10min after injection, and excreted mainly to the biliary system and the gastrointestinal tract. The clear liver imaging was obtained between 15 and 30min after injection of 99Tcm-GHSA-IFNα2b.Therefore, GHSA-IFNα2b would be a promising interferon with good liver-targeting ability. 99Tcm-GHSA-IFNα2b would be a potential hepatic receptor imaging agent.
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