Türker Selcan, Erdoğan Suna, Ozer Yekta A, Bilgili Hasan, Deveci Salih
Department of Radiopharmacy, Faculty of Pharmacy, Hacettepe University, Sihhiye, Ankara, Turkey.
J Drug Target. 2008 Jan;16(1):51-7. doi: 10.1080/10611860701725191.
Recent research into the complex and varied components of rheumatoid arthritis (RA) is leading to the development of more effective targets for pharmaceutical approach than even before. Current treatment of RA frequently includes the use of nonsteroidal anti-inflammatory drugs, such as Diclofenac sodium (DFNa) in spite of the severe adverse effects. Local application and incorporation of the drugs in liposome based formulations may reduce those side effects and improve the efficacy of drugs by reducing the availability of them in systemic circulation and increasing accumulation and retention time in the sites of inflammation. Herein, anti-inflammatory efficacy of the DFNa containing lipogelosome formulations (L1J1) was evaluated and found that L1J1 elicits a better anti-inflammatory efficacy after a single dose i.a. administration in comparison with commercial product, VE-CP, which is used topically. Histopathological examination of the opened joints showed that joints treated with L1J1, had significantly (p < 0.05) lower scores than contra lateral control joints for inflammatory changes in the synovium. These results were also confirmed by biodistribution studies.
近期对类风湿性关节炎（RA）复杂多样成分的研究正促使人们开发出比以往更有效的药物治疗靶点。尽管存在严重的副作用，但目前RA的治疗通常包括使用非甾体抗炎药，如双氯芬酸钠（DFNa）。将药物局部应用并制成基于脂质体的制剂，可能会减少这些副作用，并通过减少药物在体循环中的可用性以及增加其在炎症部位的蓄积和滞留时间来提高药物疗效。在此，对含DFNa的脂质凝胶体制剂（L1J1）的抗炎效果进行了评估，发现与局部使用的市售产品VE-CP相比，L1J1在单次关节内给药后具有更好的抗炎效果。对切开关节的组织病理学检查表明，与对侧对照关节相比，用L1J1治疗的关节滑膜炎症变化评分显著更低（p < 0.05）。生物分布研究也证实了这些结果。
