Self-microemulsifying drug delivery system for improved oral bioavailability of oleanolic acid: design and evaluation

Rui Yang,1 Xin Huang,1 Jinfeng Dou,2 Guangxi Zhai,2 Lequn Su1 1Pharmacy Department, Shandong Provincial Qianfoshan Hospital, Shandong University, Jinan, People's Republic of China; 2Department of Pharmaceutics, College of Pharmacy, Shandong University, Jinan, People's Republic of Chi...

Descripción completa

Guardado en:
Detalles Bibliográficos
Autores principales: Yang R, Huang X, Dou J, Zhai G, Su L
Formato: article
Lenguaje:EN
Publicado: Dove Medical Press 2013
Materias:
Acceso en línea:https://doaj.org/article/a5dc947a74384e2badf700f012deb160
Etiquetas: Agregar Etiqueta
Sin Etiquetas, Sea el primero en etiquetar este registro!
id oai:doaj.org-article:a5dc947a74384e2badf700f012deb160
record_format dspace
spelling oai:doaj.org-article:a5dc947a74384e2badf700f012deb1602021-12-02T02:21:19ZSelf-microemulsifying drug delivery system for improved oral bioavailability of oleanolic acid: design and evaluation1176-91141178-2013https://doaj.org/article/a5dc947a74384e2badf700f012deb1602013-08-01T00:00:00Zhttp://www.dovepress.com/1self-microemulsifying-drug-delivery-system-for-improved-oral-bio-a13951https://doaj.org/toc/1176-9114https://doaj.org/toc/1178-2013Rui Yang,1 Xin Huang,1 Jinfeng Dou,2 Guangxi Zhai,2 Lequn Su1 1Pharmacy Department, Shandong Provincial Qianfoshan Hospital, Shandong University, Jinan, People's Republic of China; 2Department of Pharmaceutics, College of Pharmacy, Shandong University, Jinan, People's Republic of China Abstract: Oleanolic acid is a poorly water-soluble drug with low oral bioavailability. A self-microemulsifying drug delivery system (SMEDDS) has been developed to enhance the solubility and oral bioavailability of oleanolic acid. The formulation design was optimized by solubility assay, compatibility tests, and pseudoternary phase diagrams. The morphology, droplet size distribution, zeta potential, viscosity, electrical conductivity, and refractive index of a SMEDDS loaded with oleanolic acid were studied in detail. Compared with oleanolic acid solution, the in vitro release of oleanolic acid from SMEDDS showed that the drug could be released in a sustained manner. A highly selective and sensitive high-performance liquid chromatography-mass spectrometry method was developed for determination of oleanolic acid in rat plasma. This method was used for a pharmacokinetic study of an oleanolic acid-loaded SMEDDS compared with the conventional tablet in rats. Promisingly, a 5.07-fold increase in oral bioavailability of oleanolic acid was achieved for the SMEDDS compared with the marketed product in tablet form. Our studies illustrate the potential use of a SMEDDS for delivery of oleanolic acid via the oral route. Keywords: oleanolic acid, self-microemulsifying drug delivery system, formulation design, in vitro release, bioavailabilityYang RHuang XDou JZhai GSu LDove Medical PressarticleMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol 2013, Iss default, Pp 2917-2926 (2013)
institution DOAJ
collection DOAJ
language EN
topic Medicine (General)
R5-920
spellingShingle Medicine (General)
R5-920
Yang R
Huang X
Dou J
Zhai G
Su L
Self-microemulsifying drug delivery system for improved oral bioavailability of oleanolic acid: design and evaluation
description Rui Yang,1 Xin Huang,1 Jinfeng Dou,2 Guangxi Zhai,2 Lequn Su1 1Pharmacy Department, Shandong Provincial Qianfoshan Hospital, Shandong University, Jinan, People's Republic of China; 2Department of Pharmaceutics, College of Pharmacy, Shandong University, Jinan, People's Republic of China Abstract: Oleanolic acid is a poorly water-soluble drug with low oral bioavailability. A self-microemulsifying drug delivery system (SMEDDS) has been developed to enhance the solubility and oral bioavailability of oleanolic acid. The formulation design was optimized by solubility assay, compatibility tests, and pseudoternary phase diagrams. The morphology, droplet size distribution, zeta potential, viscosity, electrical conductivity, and refractive index of a SMEDDS loaded with oleanolic acid were studied in detail. Compared with oleanolic acid solution, the in vitro release of oleanolic acid from SMEDDS showed that the drug could be released in a sustained manner. A highly selective and sensitive high-performance liquid chromatography-mass spectrometry method was developed for determination of oleanolic acid in rat plasma. This method was used for a pharmacokinetic study of an oleanolic acid-loaded SMEDDS compared with the conventional tablet in rats. Promisingly, a 5.07-fold increase in oral bioavailability of oleanolic acid was achieved for the SMEDDS compared with the marketed product in tablet form. Our studies illustrate the potential use of a SMEDDS for delivery of oleanolic acid via the oral route. Keywords: oleanolic acid, self-microemulsifying drug delivery system, formulation design, in vitro release, bioavailability
format article
author Yang R
Huang X
Dou J
Zhai G
Su L
author_facet Yang R
Huang X
Dou J
Zhai G
Su L
author_sort Yang R
title Self-microemulsifying drug delivery system for improved oral bioavailability of oleanolic acid: design and evaluation
title_short Self-microemulsifying drug delivery system for improved oral bioavailability of oleanolic acid: design and evaluation
title_full Self-microemulsifying drug delivery system for improved oral bioavailability of oleanolic acid: design and evaluation
title_fullStr Self-microemulsifying drug delivery system for improved oral bioavailability of oleanolic acid: design and evaluation
title_full_unstemmed Self-microemulsifying drug delivery system for improved oral bioavailability of oleanolic acid: design and evaluation
title_sort self-microemulsifying drug delivery system for improved oral bioavailability of oleanolic acid: design and evaluation
publisher Dove Medical Press
publishDate 2013
url https://doaj.org/article/a5dc947a74384e2badf700f012deb160
work_keys_str_mv AT yangr selfmicroemulsifyingdrugdeliverysystemforimprovedoralbioavailabilityofoleanolicaciddesignandevaluation
AT huangx selfmicroemulsifyingdrugdeliverysystemforimprovedoralbioavailabilityofoleanolicaciddesignandevaluation
AT douj selfmicroemulsifyingdrugdeliverysystemforimprovedoralbioavailabilityofoleanolicaciddesignandevaluation
AT zhaig selfmicroemulsifyingdrugdeliverysystemforimprovedoralbioavailabilityofoleanolicaciddesignandevaluation
AT sul selfmicroemulsifyingdrugdeliverysystemforimprovedoralbioavailabilityofoleanolicaciddesignandevaluation
_version_ 1718402545479581696