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阿苯达唑亚砜负载热敏水凝胶的表征与生物活性

Characterizations and bioactivities of abendazole sulfoxide-loaded thermo-sensitive hydrogel.

作者信息

Feng Yi, Wang Fen, Zhang Xue-Wei, Bhutani Harshit, Ye Bin

机构信息

Department of Pathogenic Biology, Chongqing Medical University, Chongqing, 400016, People's Republic of China.

Batch 2013, Clinical Medicine, College of Overseas Student, Chongqing Medical University, Chongqing, 400016, People's Republic of China.

出版信息

Parasitol Res. 2017 Mar;116(3):921-928. doi: 10.1007/s00436-016-5365-y. Epub 2016 Dec 27.

Abstract

Albendazole (ABZ), a widely used anthelmintic, attributes its primary metabolite-albendazole sulfoxide (ABZSO)-as an effective agent against helminthes. For a purpose of long-lasting releasing ABZSO in a special lesion, the present study successfully manufactured ABZSO-loaded thermo-sensitive hydrogel, which was proved by FTIR and H NMR, in the interim; in vitro and in vivo behaviors of the thermo-sensitive hydrogel containing ABZSO were studied too. The in vivo pharmacokinetics parameters indicated ABZSO-loaded hydrogel as a better choice for sustained release compared with simple ABZSO. Additionally, the effect of the prepared hydrogels against helminth was investigated by the lethality of Caenorhabditis elegans, the results indicated that the lethality of ABZSO-loaded hydrogel (1, 2, and 4 mg/ml, respectively) on C. elegans was higher than that of PLGA-PEG-PLGA group (P < 0.05). It suggested that the hydrogels loaded with albendazole sulfoxide could be considered highly effective against the nematode C. elegans.

摘要

阿苯达唑(ABZ)是一种广泛使用的驱虫药,其主要代谢产物——阿苯达唑亚砜(ABZSO)被认为是一种有效的抗蠕虫剂。为了在特定病变部位实现阿苯达唑亚砜的长效释放,本研究成功制备了载有阿苯达唑亚砜的热敏水凝胶,在此期间通过傅里叶变换红外光谱(FTIR)和核磁共振氢谱(H NMR)进行了验证;同时还研究了含阿苯达唑亚砜的热敏水凝胶的体外和体内行为。体内药代动力学参数表明,与单纯的阿苯达唑亚砜相比,载有阿苯达唑亚砜的水凝胶是更优的缓释选择。此外,通过秀丽隐杆线虫的致死率研究了所制备水凝胶对蠕虫的作用,结果表明,载有阿苯达唑亚砜的水凝胶(分别为1、2和4mg/ml)对秀丽隐杆线虫的致死率高于聚乳酸-聚乙二醇-聚乳酸(PLGA-PEG-PLGA)组(P<0.05)。这表明载有阿苯达唑亚砜的水凝胶对秀丽隐杆线虫线虫可能具有高效作用。

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