Effects of Spray-Drying and Choice of Solid Carriers on Concentrations of Labrasol® and Transcutol® in Solid Self-Microemulsifying Drug Delivery Systems (SMEDDS)

Solid self-microemulsifying drug delivery systems (SMEDDS) have been used increasingly for improving the bioavailability of hydrophobic drugs. Labrasol® and Transcutol® are used widely as surfactant and solubilizer in the formulation of solid SMEDDS. We investigated the eff...

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Main Authors: Christopher Wai-Kei Lam, Tao Yi, Liang Li
Format: Article
Language:English
Published: MDPI AG 2013-01-01
Series:Molecules
Subjects:
Online Access:http://www.mdpi.com/1420-3049/18/1/545
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author Christopher Wai-Kei Lam
Tao Yi
Liang Li
author_facet Christopher Wai-Kei Lam
Tao Yi
Liang Li
author_sort Christopher Wai-Kei Lam
collection DOAJ
description Solid self-microemulsifying drug delivery systems (SMEDDS) have been used increasingly for improving the bioavailability of hydrophobic drugs. Labrasol® and Transcutol® are used widely as surfactant and solubilizer in the formulation of solid SMEDDS. We investigated the effects of spray-drying and the use of different solid carriers on concentrations of Labrasol® and Transcutol® in solid SMEDDS with scutellarin as the formulated drug. Liquid and gas chromatography tandem mass spectrometry (LC-MS and GC-MS) methods were developed for measuring low concentrations of Labrasol® and Transcutol®. In the preparation of solid SMEDDS, lactose, hydroxypropylmethyl cellulose (HPMC) and microcrystalline cellulose (MCC) were used as solid carriers. Judging from the retention ratios of Labrasol® and Transcutol®, the droplet size of solid SMEDDS increased after spray-drying of liquid SMEDDS, and concentrations of these excipients decreased after the solidifying procedure. In such reduction, Lactose and HPMC were found to preserve Labrasol® and Transcutol® better than MCC during spray-drying, and the resultant droplet sizes were smaller than that of MCC. Labrasol® and Transcutol® showed good thermal stability at 60 °C degree for 10 days. It can be concluded that spray-drying could increase the droplet size of solid SMEDDS and decreased the concentration of Labrasol® and Transcutol® therein, while water-soluble solid carriers could preserve Labrasol® and Transcutol® better than insoluble carriers in the solid SMEDDS.
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spelling doaj.art-80417a54171048569f8deb5fb767a9a52022-12-22T00:53:35ZengMDPI AGMolecules1420-30492013-01-0118154556010.3390/molecules18010545Effects of Spray-Drying and Choice of Solid Carriers on Concentrations of Labrasol® and Transcutol® in Solid Self-Microemulsifying Drug Delivery Systems (SMEDDS)Christopher Wai-Kei LamTao YiLiang LiSolid self-microemulsifying drug delivery systems (SMEDDS) have been used increasingly for improving the bioavailability of hydrophobic drugs. Labrasol® and Transcutol® are used widely as surfactant and solubilizer in the formulation of solid SMEDDS. We investigated the effects of spray-drying and the use of different solid carriers on concentrations of Labrasol® and Transcutol® in solid SMEDDS with scutellarin as the formulated drug. Liquid and gas chromatography tandem mass spectrometry (LC-MS and GC-MS) methods were developed for measuring low concentrations of Labrasol® and Transcutol®. In the preparation of solid SMEDDS, lactose, hydroxypropylmethyl cellulose (HPMC) and microcrystalline cellulose (MCC) were used as solid carriers. Judging from the retention ratios of Labrasol® and Transcutol®, the droplet size of solid SMEDDS increased after spray-drying of liquid SMEDDS, and concentrations of these excipients decreased after the solidifying procedure. In such reduction, Lactose and HPMC were found to preserve Labrasol® and Transcutol® better than MCC during spray-drying, and the resultant droplet sizes were smaller than that of MCC. Labrasol® and Transcutol® showed good thermal stability at 60 °C degree for 10 days. It can be concluded that spray-drying could increase the droplet size of solid SMEDDS and decreased the concentration of Labrasol® and Transcutol® therein, while water-soluble solid carriers could preserve Labrasol® and Transcutol® better than insoluble carriers in the solid SMEDDS.http://www.mdpi.com/1420-3049/18/1/545solid SMEDDSspray-dryingsolid carriersexcipientsLC/GC-MS
spellingShingle Christopher Wai-Kei Lam
Tao Yi
Liang Li
Effects of Spray-Drying and Choice of Solid Carriers on Concentrations of Labrasol® and Transcutol® in Solid Self-Microemulsifying Drug Delivery Systems (SMEDDS)
Molecules
solid SMEDDS
spray-drying
solid carriers
excipients
LC/GC-MS
title Effects of Spray-Drying and Choice of Solid Carriers on Concentrations of Labrasol® and Transcutol® in Solid Self-Microemulsifying Drug Delivery Systems (SMEDDS)
title_full Effects of Spray-Drying and Choice of Solid Carriers on Concentrations of Labrasol® and Transcutol® in Solid Self-Microemulsifying Drug Delivery Systems (SMEDDS)
title_fullStr Effects of Spray-Drying and Choice of Solid Carriers on Concentrations of Labrasol® and Transcutol® in Solid Self-Microemulsifying Drug Delivery Systems (SMEDDS)
title_full_unstemmed Effects of Spray-Drying and Choice of Solid Carriers on Concentrations of Labrasol® and Transcutol® in Solid Self-Microemulsifying Drug Delivery Systems (SMEDDS)
title_short Effects of Spray-Drying and Choice of Solid Carriers on Concentrations of Labrasol® and Transcutol® in Solid Self-Microemulsifying Drug Delivery Systems (SMEDDS)
title_sort effects of spray drying and choice of solid carriers on concentrations of labrasol amp 174 and transcutol amp 174 in solid self microemulsifying drug delivery systems smedds
topic solid SMEDDS
spray-drying
solid carriers
excipients
LC/GC-MS
url http://www.mdpi.com/1420-3049/18/1/545
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AT taoyi effectsofspraydryingandchoiceofsolidcarriersonconcentrationsoflabrasolamp174andtranscutolamp174insolidselfmicroemulsifyingdrugdeliverysystemssmedds
AT liangli effectsofspraydryingandchoiceofsolidcarriersonconcentrationsoflabrasolamp174andtranscutolamp174insolidselfmicroemulsifyingdrugdeliverysystemssmedds