Solid lipid nanoparticle suspension enhanced the therapeutic efficacy of praziquantel against tapeworm

Shuyu Xie1,*, Baoliang Pan1,*, Baoxin Shi2, Zhuangzhi Zhang2, Xu Zhang2, Ming Wang1, Wenzhong Zhou11Department of Preventive Veterinary Medicine, College of Veterinary Medicine, China Agricultural University, Beijing, People&rsquo;s Republic of China; 2Veterinary Research Institute, Xinjiang...

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Autores principales:	Xie S, Pan B, Shi B, Zhang Z, Zhang X, Wang M, Zhou W
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2011
Materias:	Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/4cddc9f8ba7d4933aff60cc5f196607e
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spelling	oai:doaj.org-article:4cddc9f8ba7d4933aff60cc5f196607e2021-12-02T02:10:26ZSolid lipid nanoparticle suspension enhanced the therapeutic efficacy of praziquantel against tapeworm1176-91141178-2013https://doaj.org/article/4cddc9f8ba7d4933aff60cc5f196607e2011-10-01T00:00:00Zhttp://www.dovepress.com/solid-lipid-nanoparticle-suspension-enhanced-the-therapeutic-efficacy--a8494https://doaj.org/toc/1176-9114https://doaj.org/toc/1178-2013Shuyu Xie1,, Baoliang Pan1,, Baoxin Shi2, Zhuangzhi Zhang2, Xu Zhang2, Ming Wang1, Wenzhong Zhou11Department of Preventive Veterinary Medicine, College of Veterinary Medicine, China Agricultural University, Beijing, People&rsquo;s Republic of China; 2Veterinary Research Institute, Xinjiang Academy of Animal Science, Xinjiang, People&rsquo;s Republic of China *These authors contributed equally to this study Abstract: Hydatid disease caused by tapeworm is an increasing public health and socioeconomic concern. In order to enhance the therapeutic efficacy of praziquantel (PZQ) against tapeworm, PZQ-loaded hydrogenated castor oil solid lipid nanoparticle (PZQ-HCO-SLN) suspension was prepared by a hot homogenization and ultrasonication method. The stability of the suspension at 4&deg;C and room temperature was evaluated by the physicochemical characteristics of the nanoparticles and in-vitro release pattern of the suspension. Pharmacokinetics was studied after subcutaneous administration of the suspension in dogs. The therapeutic effect of the novel formulation was evaluated in dogs naturally infected with Echinococcus granulosus. The results showed that the drug recovery of the suspension was 97.59% &plusmn; 7.56%. Nanoparticle diameter, polydispersivity index, and zeta potential were 263.00 &plusmn; 11.15 nm, 0.34 &plusmn; 0.06, and -11.57 &plusmn; 1.12 mV, respectively and showed no significant changes after 4 months of storage at both 4&deg;C and room temperature. The stored suspensions displayed similar in-vitro release patterns as that of the newly prepared one. SLNs increased the bioavailability of PZQ 5.67-fold and extended the mean residence time of the drug from 56.71 to 280.38 hours. Single subcutaneous administration of PZQ-HCO-SLN suspension obtained enhanced therapeutic efficacy against tapeworm in infected dogs. At the dose of 5 mg/kg, the stool-ova reduction and negative conversion rates and tapeworm removal rate of the suspension were 100%, while the native PZQ were 91.55%, 87.5%, and 66.7%. When the dose reduced to 0.5 mg/kg, the native drug showed no effect, but the suspension still got the same therapeutic efficacy as that of the 5 mg/kg native PZQ. These results demonstrate that the PZQ-HCO-SLN suspension is a promising formulation to enhance the therapeutic efficacy of PZQ. Keywords: pharmacokinetics, hydatid disease, Echinococcus granulosusXie SPan BShi BZhang ZZhang XWang MZhou WDove Medical PressarticleMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol 2011, Iss default, Pp 2367-2374 (2011)
institution	DOAJ
collection	DOAJ
language	EN
topic	Medicine (General) R5-920
spellingShingle	Medicine (General) R5-920 Xie S Pan B Shi B Zhang Z Zhang X Wang M Zhou W Solid lipid nanoparticle suspension enhanced the therapeutic efficacy of praziquantel against tapeworm
description	Shuyu Xie1,, Baoliang Pan1,, Baoxin Shi2, Zhuangzhi Zhang2, Xu Zhang2, Ming Wang1, Wenzhong Zhou11Department of Preventive Veterinary Medicine, College of Veterinary Medicine, China Agricultural University, Beijing, People&rsquo;s Republic of China; 2Veterinary Research Institute, Xinjiang Academy of Animal Science, Xinjiang, People&rsquo;s Republic of China *These authors contributed equally to this study Abstract: Hydatid disease caused by tapeworm is an increasing public health and socioeconomic concern. In order to enhance the therapeutic efficacy of praziquantel (PZQ) against tapeworm, PZQ-loaded hydrogenated castor oil solid lipid nanoparticle (PZQ-HCO-SLN) suspension was prepared by a hot homogenization and ultrasonication method. The stability of the suspension at 4&deg;C and room temperature was evaluated by the physicochemical characteristics of the nanoparticles and in-vitro release pattern of the suspension. Pharmacokinetics was studied after subcutaneous administration of the suspension in dogs. The therapeutic effect of the novel formulation was evaluated in dogs naturally infected with Echinococcus granulosus. The results showed that the drug recovery of the suspension was 97.59% &plusmn; 7.56%. Nanoparticle diameter, polydispersivity index, and zeta potential were 263.00 &plusmn; 11.15 nm, 0.34 &plusmn; 0.06, and -11.57 &plusmn; 1.12 mV, respectively and showed no significant changes after 4 months of storage at both 4&deg;C and room temperature. The stored suspensions displayed similar in-vitro release patterns as that of the newly prepared one. SLNs increased the bioavailability of PZQ 5.67-fold and extended the mean residence time of the drug from 56.71 to 280.38 hours. Single subcutaneous administration of PZQ-HCO-SLN suspension obtained enhanced therapeutic efficacy against tapeworm in infected dogs. At the dose of 5 mg/kg, the stool-ova reduction and negative conversion rates and tapeworm removal rate of the suspension were 100%, while the native PZQ were 91.55%, 87.5%, and 66.7%. When the dose reduced to 0.5 mg/kg, the native drug showed no effect, but the suspension still got the same therapeutic efficacy as that of the 5 mg/kg native PZQ. These results demonstrate that the PZQ-HCO-SLN suspension is a promising formulation to enhance the therapeutic efficacy of PZQ. Keywords: pharmacokinetics, hydatid disease, Echinococcus granulosus
format	article
author	Xie S Pan B Shi B Zhang Z Zhang X Wang M Zhou W
author_facet	Xie S Pan B Shi B Zhang Z Zhang X Wang M Zhou W
author_sort	Xie S
title	Solid lipid nanoparticle suspension enhanced the therapeutic efficacy of praziquantel against tapeworm
title_short	Solid lipid nanoparticle suspension enhanced the therapeutic efficacy of praziquantel against tapeworm
title_full	Solid lipid nanoparticle suspension enhanced the therapeutic efficacy of praziquantel against tapeworm
title_fullStr	Solid lipid nanoparticle suspension enhanced the therapeutic efficacy of praziquantel against tapeworm
title_full_unstemmed	Solid lipid nanoparticle suspension enhanced the therapeutic efficacy of praziquantel against tapeworm
title_sort	solid lipid nanoparticle suspension enhanced the therapeutic efficacy of praziquantel against tapeworm
publisher	Dove Medical Press
publishDate	2011
url	https://doaj.org/article/4cddc9f8ba7d4933aff60cc5f196607e
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Solid lipid nanoparticle suspension enhanced the therapeutic efficacy of praziquantel against tapeworm

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