Characterization and evaluation of an oral microemulsion containing the antitumor diterpenoid compound ent-11alpha-hydroxy-15-oxo-kaur-16-en-19-oic-acid

Yingnian Lu,1,2 Kefeng Wu,2 Li Li,2 Yuhui He,2 Liao Cui,2 Nianci Liang,2 Bozhong Mu11Department of Chemistry, East China University of Science and Technology, Shanghai, 2Guangdong Key Laboratory for Research and Development of Natural Drugs, Guangdong Medical College, Zhanjiang, People’s R...

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Autores principales:	Lu Y, Wu K, Li L, He Y, Cui L, Liang N, Mu B
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2013
Materias:	Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/5ac1bad7020d46b9affeb66482732933
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spelling	oai:doaj.org-article:5ac1bad7020d46b9affeb664827329332021-12-02T02:28:08ZCharacterization and evaluation of an oral microemulsion containing the antitumor diterpenoid compound ent-11alpha-hydroxy-15-oxo-kaur-16-en-19-oic-acid1176-91141178-2013https://doaj.org/article/5ac1bad7020d46b9affeb664827329332013-05-01T00:00:00Zhttp://www.dovepress.com/characterization-and-evaluation-of-an-oral-microemulsion-containing-th-a13023https://doaj.org/toc/1176-9114https://doaj.org/toc/1178-2013Yingnian Lu,1,2 Kefeng Wu,2 Li Li,2 Yuhui He,2 Liao Cui,2 Nianci Liang,2 Bozhong Mu11Department of Chemistry, East China University of Science and Technology, Shanghai, 2Guangdong Key Laboratory for Research and Development of Natural Drugs, Guangdong Medical College, Zhanjiang, People’s Republic of ChinaAbstract: The objective of this study was to develop an oral microemulsion formulation of the antitumor diterpenoid agent, ent-11a-hydroxy-15-oxo-kaur-16-en-19-oic- acid (henceforth referred to as 5F), to enhance its bioavailability and evaluate its hepatotoxicity. Pseudoternary phase diagrams showed that the optimal microemulsion formulation contained 45% water, 10% castor oil as the oil phase, 15% Cremophor EL as the surfactant, and 30% as a cosurfactant mixture of 1,2-propanediol and polyethylene glycol (PEG)-400 (2:1, w/w). The microemulsion preparation was characterized and its droplet diameter was within 50 nm. Release of 5F in vitro from the microemulsion was slightly increased compared with a suspension containing the same amount of active drug. Pharmacokinetic parameters in vivo indicated that bioavailability was markedly improved, with the relative bioavailability being 616.15% higher for the microemulsion than for the suspension. Toxicity tests showed that the microemulsion had no hepatotoxicity in mice. These results suggest the potential for 5F microemulsion to be administered by the oral route.Keywords: antitumor, diterpenoid, microemulsion, pharmacokinetics, toxicityLu YWu KLi LHe YCui LLiang NMu BDove Medical PressarticleMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol 2013, Iss default, Pp 1879-1886 (2013)
institution	DOAJ
collection	DOAJ
language	EN
topic	Medicine (General) R5-920
spellingShingle	Medicine (General) R5-920 Lu Y Wu K Li L He Y Cui L Liang N Mu B Characterization and evaluation of an oral microemulsion containing the antitumor diterpenoid compound ent-11alpha-hydroxy-15-oxo-kaur-16-en-19-oic-acid
description	Yingnian Lu,1,2 Kefeng Wu,2 Li Li,2 Yuhui He,2 Liao Cui,2 Nianci Liang,2 Bozhong Mu11Department of Chemistry, East China University of Science and Technology, Shanghai, 2Guangdong Key Laboratory for Research and Development of Natural Drugs, Guangdong Medical College, Zhanjiang, People’s Republic of ChinaAbstract: The objective of this study was to develop an oral microemulsion formulation of the antitumor diterpenoid agent, ent-11a-hydroxy-15-oxo-kaur-16-en-19-oic- acid (henceforth referred to as 5F), to enhance its bioavailability and evaluate its hepatotoxicity. Pseudoternary phase diagrams showed that the optimal microemulsion formulation contained 45% water, 10% castor oil as the oil phase, 15% Cremophor EL as the surfactant, and 30% as a cosurfactant mixture of 1,2-propanediol and polyethylene glycol (PEG)-400 (2:1, w/w). The microemulsion preparation was characterized and its droplet diameter was within 50 nm. Release of 5F in vitro from the microemulsion was slightly increased compared with a suspension containing the same amount of active drug. Pharmacokinetic parameters in vivo indicated that bioavailability was markedly improved, with the relative bioavailability being 616.15% higher for the microemulsion than for the suspension. Toxicity tests showed that the microemulsion had no hepatotoxicity in mice. These results suggest the potential for 5F microemulsion to be administered by the oral route.Keywords: antitumor, diterpenoid, microemulsion, pharmacokinetics, toxicity
format	article
author	Lu Y Wu K Li L He Y Cui L Liang N Mu B
author_facet	Lu Y Wu K Li L He Y Cui L Liang N Mu B
author_sort	Lu Y
title	Characterization and evaluation of an oral microemulsion containing the antitumor diterpenoid compound ent-11alpha-hydroxy-15-oxo-kaur-16-en-19-oic-acid
title_short	Characterization and evaluation of an oral microemulsion containing the antitumor diterpenoid compound ent-11alpha-hydroxy-15-oxo-kaur-16-en-19-oic-acid
title_full	Characterization and evaluation of an oral microemulsion containing the antitumor diterpenoid compound ent-11alpha-hydroxy-15-oxo-kaur-16-en-19-oic-acid
title_fullStr	Characterization and evaluation of an oral microemulsion containing the antitumor diterpenoid compound ent-11alpha-hydroxy-15-oxo-kaur-16-en-19-oic-acid
title_full_unstemmed	Characterization and evaluation of an oral microemulsion containing the antitumor diterpenoid compound ent-11alpha-hydroxy-15-oxo-kaur-16-en-19-oic-acid
title_sort	characterization and evaluation of an oral microemulsion containing the antitumor diterpenoid compound ent-11alpha-hydroxy-15-oxo-kaur-16-en-19-oic-acid
publisher	Dove Medical Press
publishDate	2013
url	https://doaj.org/article/5ac1bad7020d46b9affeb66482732933
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Characterization and evaluation of an oral microemulsion containing the antitumor diterpenoid compound ent-11alpha-hydroxy-15-oxo-kaur-16-en-19-oic-acid

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