Hrckova G, Velebný S
Parasitological Institute, The Slovak Academy of Sciences, Kosice, Slovak Republic.
J Helminthol. 2001 Jun;75(2):141-6.
Benzimidazole carbamates (mebendazole, albendazole and fenbendazole) are the most commonly used anthelmintic drugs for the treatment of larval toxocariasis (Toxocara canis) in paratenic hosts. However, the bioavailability of these drugs for tissues is very low due to their extremely low solubility, resulting in the administration of relatively high doses over a long period. To overcome this problem, neutral, negatively or positively charged and stabilized liposome drug carriers were examined in the chronic phase of T. canis infections in mice each orally inoculated with 1000 eggs. Moreover, liposomized albendazole and fenbendazole were co-administered with liposomized immunomodulator glucan. The highest efficacy of both drugs, evaluated 4 weeks after treatment, was recorded after their subcutaneous administration (ten doses of 25 mg kg(-1)) in stabilized liposomes and intramuscular co-administration of liposomized glucan (two doses of 5 mg kg(-1)). Fenbendazole was more effective in muscles (91.5%) whereas albendazole was more effective in the brain (92.2%). Liposomes with incorporated benzimidazole carbamate anthelmintics provide sustained drug-release reservoirs and can considerably enhance drug efficacy. Moreover, despite suppression by T. canis antigens, stimulation of the immune system by the immunomodulator glucan potentiates the effects of these antiparasitic drugs.
苯并咪唑氨基甲酸盐类药物（甲苯达唑、阿苯达唑和芬苯达唑）是治疗转续宿主中幼虫型犬弓首蛔虫病（犬弓首蛔虫）最常用的驱虫药物。然而，由于这些药物的溶解度极低，其在组织中的生物利用度非常低，导致需要长期给予相对高剂量的药物。为克服这一问题，研究人员在每只经口接种1000枚虫卵的小鼠犬弓首蛔虫感染慢性期，对中性、带负电荷或正电荷以及稳定化的脂质体药物载体进行了研究。此外，将脂质体阿苯达唑和芬苯达唑与脂质体免疫调节剂葡聚糖联合给药。治疗4周后评估发现，两种药物在以稳定化脂质体皮下给药（十次剂量为25 mg kg⁻¹）并肌肉内联合给予脂质体葡聚糖（两次剂量为5 mg kg⁻¹）后疗效最高。芬苯达唑在肌肉中的疗效更高（91.5%），而阿苯达唑在脑中的疗效更高（92.2%）。载有苯并咪唑氨基甲酸盐类驱虫药的脂质体可提供持续的药物释放库，并可显著提高药物疗效。此外，尽管受到犬弓首蛔虫抗原的抑制，但免疫调节剂葡聚糖对免疫系统的刺激可增强这些抗寄生虫药物 的作用。
