Self-microemulsifying drug-delivery system for improved oral bioavailability of 20(S)-25-methoxyl-dammarane-3β, 12β, 20-triol: preparation and evaluation

Self-microemulsifying drug-delivery system for improved oral bioavailability of 20(S)-25-methoxyl-dammarane-3β, 12β, 20-triol: preparation and evaluation

Shuang Cai,1,* Cai-Hong Shi,2,* Xiangrong Zhang,2 Xiaojiao Tang,2 Hao Suo,2 Li Yang,2 Yuqing Zhao2 1Department of Pharmacy, The First Affiliated Hospital of China Medical University, 2Shenyang Pharmaceutical University, Shenyang, People's Republic of China *These authors contributed equall...

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Autores principales: Cai S, Shi CH, Zhang XR, Tang XJ, Suo H, Yang L, Zhao YQ
Formato: article
Lenguaje:EN
Publicado: Dove Medical Press 2014
Materias:
Medicine (General)
R5-920
Acceso en línea:https://doaj.org/article/53b5bdc0a84e4df6a636f93ee2983bd7
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spelling oai:doaj.org-article:53b5bdc0a84e4df6a636f93ee2983bd72021-12-02T07:28:32ZSelf-microemulsifying drug-delivery system for improved oral bioavailability of 20(S)-25-methoxyl-dammarane-3β, 12β, 20-triol: preparation and evaluation1178-2013https://doaj.org/article/53b5bdc0a84e4df6a636f93ee2983bd72014-02-01T00:00:00Zhttp://www.dovepress.com/self-microemulsifying-drug-delivery-system-for-improved-oral-bio-a15793https://doaj.org/toc/1178-2013 Shuang Cai,1,* Cai-Hong Shi,2,* Xiangrong Zhang,2 Xiaojiao Tang,2 Hao Suo,2 Li Yang,2 Yuqing Zhao2 1Department of Pharmacy, The First Affiliated Hospital of China Medical University, 2Shenyang Pharmaceutical University, Shenyang, People's Republic of China *These authors contributed equally to this work Abstract: The objective of this study was to develop a self-microemulsifying drug delivery system (SMEDDS) to enhance the oral bioavailability of the poorly water-soluble compound 20(S)-25-methoxydammarane-3β;12β;20-triol (25-OCH3-PPD). Optimized SMEDDS formulations for 25-OCH3-PPD contained Cremophor® EL (50%) as the surfactant, glycerin (20%) as the cosurfactant, and Labrafil® M1944 (30%) as the oil. The SMEDDS were characterized by morphological observation and mean droplet size. The pharmacokinetics and bioavailability of the 25-OCH3-PPD suspension and SMEDDS were evaluated and compared in rats. The plasma concentrations of 25-OCH3-PPD and its main metabolite, 25-OH-PPD, were determined by ultra performance liquid chromatography-tandem mass spectrometry. The relative bioavailability of SMEDDS was dramatically enhanced by an average of 9.8-fold compared with the suspension. Improved solubility and lymphatic transport may contribute to this enhanced bioavailability. Our studies highlight the promise of SMEDDS for the delivery of 25-OCH3-PPD via the oral route. Keywords: 25-methoxydammarane-3β;12β;20-triol (25-OCH3-PPD), 25-OH-PPD, self-microemulsifying drug delivery system, bioavailability, pharmacokineticsCai SShi CHZhang XRTang XJSuo HYang LZhao YQDove Medical PressarticleMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol 2014, Iss Issue 1, Pp 913-920 (2014)
institution DOAJ
collection DOAJ
language EN
topic Medicine (General)
R5-920
spellingShingle Medicine (General)
R5-920
Cai S
Shi CH
Zhang XR
Tang XJ
Suo H
Yang L
Zhao YQ
Self-microemulsifying drug-delivery system for improved oral bioavailability of 20(S)-25-methoxyl-dammarane-3β, 12β, 20-triol: preparation and evaluation
description Shuang Cai,1,* Cai-Hong Shi,2,* Xiangrong Zhang,2 Xiaojiao Tang,2 Hao Suo,2 Li Yang,2 Yuqing Zhao2 1Department of Pharmacy, The First Affiliated Hospital of China Medical University, 2Shenyang Pharmaceutical University, Shenyang, People's Republic of China *These authors contributed equally to this work Abstract: The objective of this study was to develop a self-microemulsifying drug delivery system (SMEDDS) to enhance the oral bioavailability of the poorly water-soluble compound 20(S)-25-methoxydammarane-3β;12β;20-triol (25-OCH3-PPD). Optimized SMEDDS formulations for 25-OCH3-PPD contained Cremophor® EL (50%) as the surfactant, glycerin (20%) as the cosurfactant, and Labrafil® M1944 (30%) as the oil. The SMEDDS were characterized by morphological observation and mean droplet size. The pharmacokinetics and bioavailability of the 25-OCH3-PPD suspension and SMEDDS were evaluated and compared in rats. The plasma concentrations of 25-OCH3-PPD and its main metabolite, 25-OH-PPD, were determined by ultra performance liquid chromatography-tandem mass spectrometry. The relative bioavailability of SMEDDS was dramatically enhanced by an average of 9.8-fold compared with the suspension. Improved solubility and lymphatic transport may contribute to this enhanced bioavailability. Our studies highlight the promise of SMEDDS for the delivery of 25-OCH3-PPD via the oral route. Keywords: 25-methoxydammarane-3β;12β;20-triol (25-OCH3-PPD), 25-OH-PPD, self-microemulsifying drug delivery system, bioavailability, pharmacokinetics
format article
author Cai S
Shi CH
Zhang XR
Tang XJ
Suo H
Yang L
Zhao YQ
author_facet Cai S
Shi CH
Zhang XR
Tang XJ
Suo H
Yang L
Zhao YQ
author_sort Cai S
title Self-microemulsifying drug-delivery system for improved oral bioavailability of 20(S)-25-methoxyl-dammarane-3β, 12β, 20-triol: preparation and evaluation
title_short Self-microemulsifying drug-delivery system for improved oral bioavailability of 20(S)-25-methoxyl-dammarane-3β, 12β, 20-triol: preparation and evaluation
title_full Self-microemulsifying drug-delivery system for improved oral bioavailability of 20(S)-25-methoxyl-dammarane-3β, 12β, 20-triol: preparation and evaluation
title_fullStr Self-microemulsifying drug-delivery system for improved oral bioavailability of 20(S)-25-methoxyl-dammarane-3β, 12β, 20-triol: preparation and evaluation
title_full_unstemmed Self-microemulsifying drug-delivery system for improved oral bioavailability of 20(S)-25-methoxyl-dammarane-3β, 12β, 20-triol: preparation and evaluation
title_sort self-microemulsifying drug-delivery system for improved oral bioavailability of 20(s)-25-methoxyl-dammarane-3β, 12β, 20-triol: preparation and evaluation
publisher Dove Medical Press
publishDate 2014
url https://doaj.org/article/53b5bdc0a84e4df6a636f93ee2983bd7
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