左旋吡喹酮脂质体及吡喹酮脂质体治疗小鼠血吸虫病

Levo-praziquantal Liposome and Praziquantel Liposome Therapy of Schistosomiasis in Mice

本研究用逆道相蒸发法制备左旋吡喹酮脂质体和吡喹酮脂质体。左旋吡喹酮脂质低（L－PZQL）和吡喹酮脂质体（PZQL）剂量均为25和50mg／kg／次，吡喹酮（PZQ）剂量为100和200mg／kg／次，以一次灌胃连续两日治疗小鼠血吸虫病。L－PZQL50mg／kg和100mg／kg治疗组减虫率分别为551％和74．5％，PZQL50mg／kg和100mg／kg治疗组减虫率分别为20．9％和55．7％，同剂量的L－PZQL与PZQL组减虫率比较有显著性差异（P＜0．01）。PZQ200mg／kg、400mg／kg组减虫率分别为59．2％和79．1％。L－PZQL疗效较PZQ高4倍。形态学观察，化疗后血吸虫成虫皮层受损害，以L－PZQL100mg／kg组和PZQ400mg／kg组尤为明显。肝脏病理学改变提示，脂质体药物组与对照组相比，肝脏嗜酸性由芽肿减少，以慢性虫卵结节居多，虫卵结书直径变小。实验说明，L－PZQL100mg／kg治疗小鼠血吸虫病的疗效类似于PZQ400mg／kg。

Levo-praziquantel liposome and praziquantel liposome were prepared by a reverse phase evaporation method. The encapsulated rate was over 98. 21%. Mice infected with schistosome japonica were treated intergastrically with L-PZQL in dose of 25 and 50mg/kg,daily,consecutive 2 days. The worm reduction rates were 55. 1% and 74.5 %,while those of PZQL at same dosage were 20.9% and 55.7%,respectively. There was difference between L-PQZL and PZQL groups (P＜0. 01). The rates in PZQ 200mg/kg and 400mg/kg groups were 59.2% and 79.1%,respctively. The efficacy of L-PZQL was higher 4 times than that of PZQ. In morpholoy the worms were shortened and tegument lesions was obvious especially in L-PZQL 100mg/kg and PZQL 400mg/kg groups. In pathological examination the liver from the treated mice were observed that the number of eosinophilic abscess were reduced and its diameter also were lessened,therfore,fibrous granuloma were remarkablely increased in L-PZQL 100mg/kg group.The results suggested that the efficacy of L-PZQL 100mg/kg should be similar to dosage of PZQ 400mg/kg in the treatment of schistosomiasis in mice.