Pharmacokinetics and enhanced oral bioavailability in beagle dogs of cyclosporine A encapsulated in glyceryl monooleate/poloxamer 407 cubic nanoparticles

Jie Lai1,2, Yi Lu1, Zongning Yin2, Fuqiang Hu3, Wei Wu11School of Pharmacy, Fudan University, Shanghai, China, 2West China School of Pharmacy, Sichuan University, Chengdu, China, 3School of Pharmacy, Zhejiang University, Hangzhou, ChinaAbstract: Efforts to improve the oral bioavailability of cyclosp...

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Autores principales:	Jie Lai, Yi Lu, Zongning Yin, et al
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2009
Materias:	Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/4c399b2ae32443b1bb1f4b36cac0d1f6
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spelling	oai:doaj.org-article:4c399b2ae32443b1bb1f4b36cac0d1f62021-12-02T05:39:39ZPharmacokinetics and enhanced oral bioavailability in beagle dogs of cyclosporine A encapsulated in glyceryl monooleate/poloxamer 407 cubic nanoparticles1176-91141178-2013https://doaj.org/article/4c399b2ae32443b1bb1f4b36cac0d1f62009-12-01T00:00:00Zhttp://www.dovepress.com/pharmacokinetics-and-enhanced-oral-bioavailability-in-beagle-dogs-of-c-a3842https://doaj.org/toc/1176-9114https://doaj.org/toc/1178-2013Jie Lai1,2, Yi Lu1, Zongning Yin2, Fuqiang Hu3, Wei Wu11School of Pharmacy, Fudan University, Shanghai, China, 2West China School of Pharmacy, Sichuan University, Chengdu, China, 3School of Pharmacy, Zhejiang University, Hangzhou, ChinaAbstract: Efforts to improve the oral bioavailability of cyclosporine A (CyA) remains a challenge in the field of drug delivery. In this study, glyceryl monooleate (GMO)/poloxamer 407 cubic nanoparticles were evaluated as potential vehicles to improve the oral bioavailability of CyA. Cubic nanoparticles were prepared via the fragmentation of a bulk GMO/poloxamer 407 cubic phase gel by sonication and homogenization. The cubic inner structure formed was verified using Cryo-TEM. The mean diameters of the nanoparticles were about 180 nm, and the entrapment efficiency of these particles for CyA was over 85%. The in vitro release of CyA from these nanoparticles was less than 5% at 12 h. The results of a pharmacokinetic study in beagle dogs showed improved absorption of CyA from cubic nanoparticles as compared to microemulsion-based Neoral&reg;; higher Cmax (1371.18 &plusmn; 37.34 vs 969.68 &plusmn; 176.3 ng mL-1), higher AUC0&ndash;t (7757.21 &plusmn; 1093.64 vs 4739.52 &plusmn; 806.30 ng h mL-1) and AUC0&ndash;&infin; (9004.77 &plusmn; 1090.38 vs 5462.31 &plusmn; 930.76 ng h mL-1). The relative oral bioavailability of CyA cubic nanoparticles calculated on the basis of AUC0&ndash;&infin; was about 178% as compared to Neoral&reg;. The enhanced bioavailability of CyA is likely due to facilitated absorption by cubic nanoparticles rather than improved release.Keywords: nanoparticles, cubosomes, cyclosporine A, glyceryl monooleate, oral drug delivery, bioavailability, beagle dogs Jie LaiYi LuZongning Yinet alDove Medical PressarticleMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol 2010, Iss default, Pp 13-23 (2009)
institution	DOAJ
collection	DOAJ
language	EN
topic	Medicine (General) R5-920
spellingShingle	Medicine (General) R5-920 Jie Lai Yi Lu Zongning Yin et al Pharmacokinetics and enhanced oral bioavailability in beagle dogs of cyclosporine A encapsulated in glyceryl monooleate/poloxamer 407 cubic nanoparticles
description	Jie Lai1,2, Yi Lu1, Zongning Yin2, Fuqiang Hu3, Wei Wu11School of Pharmacy, Fudan University, Shanghai, China, 2West China School of Pharmacy, Sichuan University, Chengdu, China, 3School of Pharmacy, Zhejiang University, Hangzhou, ChinaAbstract: Efforts to improve the oral bioavailability of cyclosporine A (CyA) remains a challenge in the field of drug delivery. In this study, glyceryl monooleate (GMO)/poloxamer 407 cubic nanoparticles were evaluated as potential vehicles to improve the oral bioavailability of CyA. Cubic nanoparticles were prepared via the fragmentation of a bulk GMO/poloxamer 407 cubic phase gel by sonication and homogenization. The cubic inner structure formed was verified using Cryo-TEM. The mean diameters of the nanoparticles were about 180 nm, and the entrapment efficiency of these particles for CyA was over 85%. The in vitro release of CyA from these nanoparticles was less than 5% at 12 h. The results of a pharmacokinetic study in beagle dogs showed improved absorption of CyA from cubic nanoparticles as compared to microemulsion-based Neoral&reg;; higher Cmax (1371.18 &plusmn; 37.34 vs 969.68 &plusmn; 176.3 ng mL-1), higher AUC0&ndash;t (7757.21 &plusmn; 1093.64 vs 4739.52 &plusmn; 806.30 ng h mL-1) and AUC0&ndash;&infin; (9004.77 &plusmn; 1090.38 vs 5462.31 &plusmn; 930.76 ng h mL-1). The relative oral bioavailability of CyA cubic nanoparticles calculated on the basis of AUC0&ndash;&infin; was about 178% as compared to Neoral&reg;. The enhanced bioavailability of CyA is likely due to facilitated absorption by cubic nanoparticles rather than improved release.Keywords: nanoparticles, cubosomes, cyclosporine A, glyceryl monooleate, oral drug delivery, bioavailability, beagle dogs
format	article
author	Jie Lai Yi Lu Zongning Yin et al
author_facet	Jie Lai Yi Lu Zongning Yin et al
author_sort	Jie Lai
title	Pharmacokinetics and enhanced oral bioavailability in beagle dogs of cyclosporine A encapsulated in glyceryl monooleate/poloxamer 407 cubic nanoparticles
title_short	Pharmacokinetics and enhanced oral bioavailability in beagle dogs of cyclosporine A encapsulated in glyceryl monooleate/poloxamer 407 cubic nanoparticles
title_full	Pharmacokinetics and enhanced oral bioavailability in beagle dogs of cyclosporine A encapsulated in glyceryl monooleate/poloxamer 407 cubic nanoparticles
title_fullStr	Pharmacokinetics and enhanced oral bioavailability in beagle dogs of cyclosporine A encapsulated in glyceryl monooleate/poloxamer 407 cubic nanoparticles
title_full_unstemmed	Pharmacokinetics and enhanced oral bioavailability in beagle dogs of cyclosporine A encapsulated in glyceryl monooleate/poloxamer 407 cubic nanoparticles
title_sort	pharmacokinetics and enhanced oral bioavailability in beagle dogs of cyclosporine a encapsulated in glyceryl monooleate/poloxamer 407 cubic nanoparticles
publisher	Dove Medical Press
publishDate	2009
url	https://doaj.org/article/4c399b2ae32443b1bb1f4b36cac0d1f6
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Pharmacokinetics and enhanced oral bioavailability in beagle dogs of cyclosporine A encapsulated in glyceryl monooleate/poloxamer 407 cubic nanoparticles

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