Supersaturable solid self-microemulsifying drug delivery system: precipitation inhibition and bioavailability enhancement

Guilan Quan,1 Boyi Niu,1 Vikramjeet Singh,1 Yixian Zhou,1 Chuan-Yu Wu,2 Xin Pan,1 Chuanbin Wu1 1School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou, China; 2Department of Chemical and Process Engineering, University of Surrey, Guildford, UK Abstract: Solid self-emulsifying drug de...

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Autores principales:	Quan G, Niu B, Singh V, Zhou Y, Wu C, Pan X
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2017
Materias:	Soluplus® supersaturation fenofibrate mesoporous silica solid self-emulsifying drug delivery system Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/e64e42a139f74ee88b65350c569ff5f9
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spelling	oai:doaj.org-article:e64e42a139f74ee88b65350c569ff5f92021-12-02T05:40:29ZSupersaturable solid self-microemulsifying drug delivery system: precipitation inhibition and bioavailability enhancement1178-2013https://doaj.org/article/e64e42a139f74ee88b65350c569ff5f92017-12-01T00:00:00Zhttps://www.dovepress.com/supersaturable-solid-self-microemulsifying-drug-delivery-system-precip-peer-reviewed-article-IJNhttps://doaj.org/toc/1178-2013Guilan Quan,1 Boyi Niu,1 Vikramjeet Singh,1 Yixian Zhou,1 Chuan-Yu Wu,2 Xin Pan,1 Chuanbin Wu1 1School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou, China; 2Department of Chemical and Process Engineering, University of Surrey, Guildford, UK Abstract: Solid self-emulsifying drug delivery system (SSEDDS), which incorporates liquid SEDDS into a solid dosage form, has been recently introduced to improve the oral bioavailability of poorly water-soluble drugs. However, supersaturated drug generated by SSEDDS is thermodynamically unstable and tends to precipitate rapidly prior to absorption, resulting in compromised bioavailability. The aim of this study was to construct a novel supersaturated SSEDDS (super-SSEDDS) by combining SSEDDS with appropriate precipitation inhibitor. Fenofibrate (FNB), a sparingly soluble drug, was selected as a model drug in this study. An optimized SSEDDS was prepared by solvent evaporation by using mesoporous silica Santa Barbara Amorphous-15 as the inert carrier. Supersaturation assay was conducted to evaluate the precipitation inhibition capacity of different polymers, and the results showed that Soluplus® could retard the FNB precipitation more effectively and sustain a higher apparent concentration for ~120 min. This effect was also clearly observed in the dissolution profiles of FNB from SSEDDS under supersaturated condition. The study of the mechanism suggested that the inhibition effect might be achieved both thermodynamically and kinetically. The area under the concentration–time curve of the super-SSEDDS was 1.4-fold greater than that of SSEDDS in the absence of Soluplus, based on an in vivo pharmacokinetic study conducted in beagle dogs. This study has demonstrated that the approach of combining SSEDDS with Soluplus as a supersaturation stabilizer constitutes a potential tool to improve the absorption of poorly water-soluble drugs. Keywords: Soluplus, supersaturation, fenofibrate, mesoporous silica, poorly water-soluble drugs Quan GNiu BSingh VZhou YWu CPan XWu CDove Medical PressarticleSoluplus®supersaturationfenofibratemesoporous silicasolid self-emulsifying drug delivery systemMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol Volume 12, Pp 8801-8811 (2017)
institution	DOAJ
collection	DOAJ
language	EN
topic	Soluplus® supersaturation fenofibrate mesoporous silica solid self-emulsifying drug delivery system Medicine (General) R5-920
spellingShingle	Soluplus® supersaturation fenofibrate mesoporous silica solid self-emulsifying drug delivery system Medicine (General) R5-920 Quan G Niu B Singh V Zhou Y Wu C Pan X Wu C Supersaturable solid self-microemulsifying drug delivery system: precipitation inhibition and bioavailability enhancement
description	Guilan Quan,1 Boyi Niu,1 Vikramjeet Singh,1 Yixian Zhou,1 Chuan-Yu Wu,2 Xin Pan,1 Chuanbin Wu1 1School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou, China; 2Department of Chemical and Process Engineering, University of Surrey, Guildford, UK Abstract: Solid self-emulsifying drug delivery system (SSEDDS), which incorporates liquid SEDDS into a solid dosage form, has been recently introduced to improve the oral bioavailability of poorly water-soluble drugs. However, supersaturated drug generated by SSEDDS is thermodynamically unstable and tends to precipitate rapidly prior to absorption, resulting in compromised bioavailability. The aim of this study was to construct a novel supersaturated SSEDDS (super-SSEDDS) by combining SSEDDS with appropriate precipitation inhibitor. Fenofibrate (FNB), a sparingly soluble drug, was selected as a model drug in this study. An optimized SSEDDS was prepared by solvent evaporation by using mesoporous silica Santa Barbara Amorphous-15 as the inert carrier. Supersaturation assay was conducted to evaluate the precipitation inhibition capacity of different polymers, and the results showed that Soluplus® could retard the FNB precipitation more effectively and sustain a higher apparent concentration for ~120 min. This effect was also clearly observed in the dissolution profiles of FNB from SSEDDS under supersaturated condition. The study of the mechanism suggested that the inhibition effect might be achieved both thermodynamically and kinetically. The area under the concentration–time curve of the super-SSEDDS was 1.4-fold greater than that of SSEDDS in the absence of Soluplus, based on an in vivo pharmacokinetic study conducted in beagle dogs. This study has demonstrated that the approach of combining SSEDDS with Soluplus as a supersaturation stabilizer constitutes a potential tool to improve the absorption of poorly water-soluble drugs. Keywords: Soluplus, supersaturation, fenofibrate, mesoporous silica, poorly water-soluble drugs
format	article
author	Quan G Niu B Singh V Zhou Y Wu C Pan X Wu C
author_facet	Quan G Niu B Singh V Zhou Y Wu C Pan X Wu C
author_sort	Quan G
title	Supersaturable solid self-microemulsifying drug delivery system: precipitation inhibition and bioavailability enhancement
title_short	Supersaturable solid self-microemulsifying drug delivery system: precipitation inhibition and bioavailability enhancement
title_full	Supersaturable solid self-microemulsifying drug delivery system: precipitation inhibition and bioavailability enhancement
title_fullStr	Supersaturable solid self-microemulsifying drug delivery system: precipitation inhibition and bioavailability enhancement
title_full_unstemmed	Supersaturable solid self-microemulsifying drug delivery system: precipitation inhibition and bioavailability enhancement
title_sort	supersaturable solid self-microemulsifying drug delivery system: precipitation inhibition and bioavailability enhancement
publisher	Dove Medical Press
publishDate	2017
url	https://doaj.org/article/e64e42a139f74ee88b65350c569ff5f9
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_version_	1718400327219150848

Supersaturable solid self-microemulsifying drug delivery system: precipitation inhibition and bioavailability enhancement

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