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载 albendazole 亚砜(ABZ-SO)壳聚糖-PLGA 纳米粒治疗实验鼠包虫病的疗效评价。

Evaluation of the efficacy of albendazole sulfoxide (ABZ-SO)-loaded chitosan-PLGA nanoparticles in the treatment of cystic echinococcosis in laboratory mice.

机构信息

Department of Parasitology, Division of Pathobiology, School of Veterinary Medicine, Shiraz University, Shiraz, 713451731, Iran.

Department of Pharmaceutical Nanotechnology, Center for Nanotechnology in Drug Delivery, School of Pharmacy, Shiraz University of Medical Sciences, Shiraz, Iran.

出版信息

Parasitol Res. 2020 Dec;119(12):4233-4241. doi: 10.1007/s00436-020-06901-2. Epub 2020 Sep 30.

DOI:10.1007/s00436-020-06901-2
PMID:32996050
Abstract

Albendazole is known as the drug of choice for medical treatment of cystic echinococcosis (CE). Albendazole sulfoxide (ABZ-SO), as the main active metabolite of albendazole, has low efficacy in the disease due to low water solubility and poor absorptivity. PLGA nanoparticles (NPs) enhance the dissolution of poorly soluble drugs, and chitosan (CS) coating enhances oral drug delivery of NPs. In this study, the efficacy of ABZ-SO-loaded CS-PGLA NPs in the treatment of CE was evaluated in laboratory mice. ABZ-SO-loaded CS-PGLA NPs were prepared by nanoprecipitation and characterized by dynamic light scattering method and scanning electron microscopy. Thirty mice were intraperitoneally infected by 1000 protoscoleces of Echinococcus granulosus. Ten months later, the mice were allocated into 3 groups: groups 1 and 2 were treated with ABZ-SO and ABZ-SO-loaded CS-PGLA NPs, respectively, and the mice in group 3 remained untreated as the control group. The drugs were administered by gavage for 45 days at a daily dose of 10 mg/kg. Finally, all mice were opened and the cysts were collected, counted, weighed, and measured separately. The therapeutic effect of ABZ-SO in the number, weight, and volume of the cysts were not statistically significant compared with those in ABZ-SO-loaded CS-PGLA NPs and the control group. However, the therapeutic effect of ABZ-SO-loaded CS-PGLA NPs in the weight and volume of cysts were statistically significant when compared with that in the control group (p ˂ 0.05). In conclusions, this study revealed that ABZ-SO-loaded CS-PGLA NPs could enhance the therapeutic efficacy of ABZ-SO in the treatment of CE in laboratory mice.

摘要

阿苯达唑是治疗囊型包虫病(CE)的首选药物。阿苯达唑砜(ABZ-SO)作为阿苯达唑的主要活性代谢物,由于其水溶性低和吸收性差,在该疾病中的疗效较低。PLGA 纳米粒(NPs)可提高难溶性药物的溶解度,壳聚糖(CS)包衣可增强 NPs 的口服药物递送。本研究评估了载 ABZ-SO 的 CS-PGLA NPs 在实验小鼠 CE 治疗中的疗效。通过纳米沉淀法制备载 ABZ-SO 的 CS-PGLA NPs,并用动态光散射法和扫描电子显微镜进行了表征。30 只小鼠经腹腔感染 1000 个细粒棘球蚴原头蚴。10 个月后,将小鼠分为 3 组:1 组和 2 组分别用 ABZ-SO 和载 ABZ-SO 的 CS-PGLA NPs 治疗,第 3 组未治疗作为对照组。药物通过灌胃给药,每日剂量为 10mg/kg,共 45 天。最后,所有小鼠均被打开,收集、计数、称重并分别测量囊肿。与载 ABZ-SO 的 CS-PGLA NPs 和对照组相比,ABZ-SO 在囊肿数量、重量和体积方面的治疗效果无统计学意义。然而,与对照组相比,载 ABZ-SO 的 CS-PGLA NPs 在囊肿重量和体积方面的治疗效果具有统计学意义(p ˂ 0.05)。综上所述,本研究表明载 ABZ-SO 的 CS-PGLA NPs 可增强 ABZ-SO 治疗实验小鼠 CE 的疗效。

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