Formulation and In Vivo Evaluation of a Solid Self-Emulsifying Drug Delivery System Using Oily Liquid Tocotrienols as Model Active Substance

Self-emulsifying drug delivery systems (SEDDS) can improve the oral bioavailability of poorly water-soluble drugs. Solid self-emulsifying drug delivery systems (s-SEDDS) offer several advantages including improved drug stability, ease of administration, and production. Most compounds employed in dev...

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Autores principales:	You Zhuan Lee, Eng Kwong Seow, Sheau Chin Lim, Kah Hay Yuen, Nurzalina Abdul Karim Khan
Formato:	article
Lenguaje:	EN
Publicado:	MDPI AG 2021
Materias:	self-emulsifying drug delivery system poorly water-soluble drugs solid dosage forms in vivo oral bioavailability pharmacokinetic tocotrienols Pharmacy and materia medica RS1-441
Acceso en línea:	https://doaj.org/article/4bc8443fe1ca49f6b03c5e464861f2bd
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spelling	oai:doaj.org-article:4bc8443fe1ca49f6b03c5e464861f2bd2021-11-25T18:40:36ZFormulation and In Vivo Evaluation of a Solid Self-Emulsifying Drug Delivery System Using Oily Liquid Tocotrienols as Model Active Substance10.3390/pharmaceutics131117771999-4923https://doaj.org/article/4bc8443fe1ca49f6b03c5e464861f2bd2021-10-01T00:00:00Zhttps://www.mdpi.com/1999-4923/13/11/1777https://doaj.org/toc/1999-4923Self-emulsifying drug delivery systems (SEDDS) can improve the oral bioavailability of poorly water-soluble drugs. Solid self-emulsifying drug delivery systems (s-SEDDS) offer several advantages including improved drug stability, ease of administration, and production. Most compounds employed in developing s-SEDDS are solid in nature, with a high amount of surfactants added. The aim of this study was to develop an s-SEDDS using a tocotrienol-rich fraction (TRF) as the model liquid active substance via a simple adsorption method. The solid formulation was developed using magnesium aluminosilicate as the carrier with 70% TRF and 30% surfactants (poloxamer and Labrasol<sup>®</sup>). The formulation showed good self-emulsification efficiency with stable emulsion formed, excellent powder flowability, and small emulsion droplet size of 210–277 nm. The s-SEDDS with combined surfactants (poloxamer and Labrasol<sup>®</sup>) showed a faster absorption rate compared to preparations with only a single surfactant and enhanced oral bioavailability (3.4–3.8 times higher) compared to the non-self-emulsifying oily preparation when administered at a fasted state in rats. In conclusion, an s-SEDDS containing a high amount of TRF was successfully developed. It may serve as a useful alternative to a liquid product with enhanced oral bioavailability and the added advantage of being a solid dosage form.You Zhuan LeeEng Kwong SeowSheau Chin LimKah Hay YuenNurzalina Abdul Karim KhanMDPI AGarticleself-emulsifying drug delivery systempoorly water-soluble drugssolid dosage formsin vivo oral bioavailabilitypharmacokinetictocotrienolsPharmacy and materia medicaRS1-441ENPharmaceutics, Vol 13, Iss 1777, p 1777 (2021)
institution	DOAJ
collection	DOAJ
language	EN
topic	self-emulsifying drug delivery system poorly water-soluble drugs solid dosage forms in vivo oral bioavailability pharmacokinetic tocotrienols Pharmacy and materia medica RS1-441
spellingShingle	self-emulsifying drug delivery system poorly water-soluble drugs solid dosage forms in vivo oral bioavailability pharmacokinetic tocotrienols Pharmacy and materia medica RS1-441 You Zhuan Lee Eng Kwong Seow Sheau Chin Lim Kah Hay Yuen Nurzalina Abdul Karim Khan Formulation and In Vivo Evaluation of a Solid Self-Emulsifying Drug Delivery System Using Oily Liquid Tocotrienols as Model Active Substance
description	Self-emulsifying drug delivery systems (SEDDS) can improve the oral bioavailability of poorly water-soluble drugs. Solid self-emulsifying drug delivery systems (s-SEDDS) offer several advantages including improved drug stability, ease of administration, and production. Most compounds employed in developing s-SEDDS are solid in nature, with a high amount of surfactants added. The aim of this study was to develop an s-SEDDS using a tocotrienol-rich fraction (TRF) as the model liquid active substance via a simple adsorption method. The solid formulation was developed using magnesium aluminosilicate as the carrier with 70% TRF and 30% surfactants (poloxamer and Labrasol<sup>®</sup>). The formulation showed good self-emulsification efficiency with stable emulsion formed, excellent powder flowability, and small emulsion droplet size of 210–277 nm. The s-SEDDS with combined surfactants (poloxamer and Labrasol<sup>®</sup>) showed a faster absorption rate compared to preparations with only a single surfactant and enhanced oral bioavailability (3.4–3.8 times higher) compared to the non-self-emulsifying oily preparation when administered at a fasted state in rats. In conclusion, an s-SEDDS containing a high amount of TRF was successfully developed. It may serve as a useful alternative to a liquid product with enhanced oral bioavailability and the added advantage of being a solid dosage form.
format	article
author	You Zhuan Lee Eng Kwong Seow Sheau Chin Lim Kah Hay Yuen Nurzalina Abdul Karim Khan
author_facet	You Zhuan Lee Eng Kwong Seow Sheau Chin Lim Kah Hay Yuen Nurzalina Abdul Karim Khan
author_sort	You Zhuan Lee
title	Formulation and In Vivo Evaluation of a Solid Self-Emulsifying Drug Delivery System Using Oily Liquid Tocotrienols as Model Active Substance
title_short	Formulation and In Vivo Evaluation of a Solid Self-Emulsifying Drug Delivery System Using Oily Liquid Tocotrienols as Model Active Substance
title_full	Formulation and In Vivo Evaluation of a Solid Self-Emulsifying Drug Delivery System Using Oily Liquid Tocotrienols as Model Active Substance
title_fullStr	Formulation and In Vivo Evaluation of a Solid Self-Emulsifying Drug Delivery System Using Oily Liquid Tocotrienols as Model Active Substance
title_full_unstemmed	Formulation and In Vivo Evaluation of a Solid Self-Emulsifying Drug Delivery System Using Oily Liquid Tocotrienols as Model Active Substance
title_sort	formulation and in vivo evaluation of a solid self-emulsifying drug delivery system using oily liquid tocotrienols as model active substance
publisher	MDPI AG
publishDate	2021
url	https://doaj.org/article/4bc8443fe1ca49f6b03c5e464861f2bd
work_keys_str_mv	AT youzhuanlee formulationandinvivoevaluationofasolidselfemulsifyingdrugdeliverysystemusingoilyliquidtocotrienolsasmodelactivesubstance AT engkwongseow formulationandinvivoevaluationofasolidselfemulsifyingdrugdeliverysystemusingoilyliquidtocotrienolsasmodelactivesubstance AT sheauchinlim formulationandinvivoevaluationofasolidselfemulsifyingdrugdeliverysystemusingoilyliquidtocotrienolsasmodelactivesubstance AT kahhayyuen formulationandinvivoevaluationofasolidselfemulsifyingdrugdeliverysystemusingoilyliquidtocotrienolsasmodelactivesubstance AT nurzalinaabdulkarimkhan formulationandinvivoevaluationofasolidselfemulsifyingdrugdeliverysystemusingoilyliquidtocotrienolsasmodelactivesubstance
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Formulation and In Vivo Evaluation of a Solid Self-Emulsifying Drug Delivery System Using Oily Liquid Tocotrienols as Model Active Substance

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