醋酸曲安奈德温敏凝胶药效学及滞留性

目的：制备关节腔注射用醋酸曲安奈德TAA温敏凝胶，考察其药效学和滞留性。方法：采用物理混合法制得TAA温敏凝胶，建立老鼠皮下气囊炎症模型，给予不同组分药物治疗后，通过对比皮下囊物理特征、组织切片的相关评价以及elisa试剂盒检测炎性因子TNF-α水平等来考察所制备的TAA温敏凝胶药效学及缓释性能，并通过小动物活体成像实验评价其滞留性。结果：药效学结果显示制备的TAA温敏凝胶相比于市售TAA混悬液对于气囊滑膜炎模型的炎症抑制作用更强、作用时间更持久。小动物活体成像实验结果显示制备的TAA温敏凝胶在体内滞留时间能达到9 d以上，能够达到缓释药物的目的，适用于关节腔局部用药的要求。结论：所制备的TAA温敏凝胶的炎症抑制作用强且持久，缓释效果及滞留性良好，有望成为新的关节腔给药传递系统。

Pharmacodynamics and retention of triamcinolone acetonide acetate thermosensitive hydrogel

OBJECTIVE To prepare triamcinolone acetonide acetate(TAA) thermosensitive hydrogel for intra-articular injection and investigate its pharmacodynamics and retention.METHODS TAA thermosensitive hydrogel was prepared with physical mixing method and through mouse subcutaneous air bag inflammation model. Different components of drug were administered to investigate their pharmacodynamics and slow-release performance by comparing physical characteristics, tissue sections and levels of inflammatory cytokine TNF-α. Moreover, small animal in vivo imaging experiments were used to evaluate their retention.RESULTS Results of pharmacodynamics showed that TAA thermosensitive hydrogel had stronger and longer inflammation inhibiting effects than TAA commercially available suspension preparation. Small animal in vivo imaging experimental results showed that TAA thermosensitive hydrogel had a retention time as long as more than 9 days in body. Therefore it was very appropriate for intra-articular injection to achieve local slow-release.CONCLUSION Inflammation inhibition of TAA thermosensitive hydrogel is strong and durable, with good slow-release and retention, and is expected to become a new drug delivery system for intra-articular injection.