In situ monitoring of the structural change of microemulsions in simulated gastrointestinal conditions by SAXS and FRET

Microemulsions are promising drug delivery systems for the oral administration of poorly water-soluble drugs. However, the evolution of microemulsions in the gastrointestinal tract is still poorly characterized, especially the structural change of microemulsions under the effect of lipase and mucus....

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Main Authors: Xia Lv, Shuguang Zhang, Huipeng Ma, Peipei Dong, Xiaodong Ma, Ming Xu, Yan Tian, Zeyao Tang, Jinyong Peng, Haibo Chen, Jianbin Zhang
Format: Article
Language:English
Published: Elsevier 2018-07-01
Series:Acta Pharmaceutica Sinica B
Online Access:http://www.sciencedirect.com/science/article/pii/S2211383517306846
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author Xia Lv
Shuguang Zhang
Huipeng Ma
Peipei Dong
Xiaodong Ma
Ming Xu
Yan Tian
Zeyao Tang
Jinyong Peng
Haibo Chen
Jianbin Zhang
author_facet Xia Lv
Shuguang Zhang
Huipeng Ma
Peipei Dong
Xiaodong Ma
Ming Xu
Yan Tian
Zeyao Tang
Jinyong Peng
Haibo Chen
Jianbin Zhang
author_sort Xia Lv
collection DOAJ
description Microemulsions are promising drug delivery systems for the oral administration of poorly water-soluble drugs. However, the evolution of microemulsions in the gastrointestinal tract is still poorly characterized, especially the structural change of microemulsions under the effect of lipase and mucus. To better understand the fate of microemulsions in the gastrointestinal tract, we applied small-angle X-ray scattering (SAXS) and fluorescence resonance energy transfer (FRET) to monitor the structural change of microemulsions under the effect of lipolysis and mucus. First, the effect of lipolysis on microemulsions was studied by SAXS, which found the generation of liquid crystalline phases. Meanwhile, FRET spectra indicated micelles with smaller particle sizes were generated during lipolysis, which could be affected by CaCl2, bile salts and lecithin. Then, the effect of mucus on the structural change of lipolysed microemulsions was studied. The results of SAXS and FRET indicated that the liquid crystalline phases disappeared, and more micelles were generated. In summary, we studied the structural change of microemulsions in simulated gastrointestinal conditions by SAXS and FRET, and successfully monitored the appearance and disappearance of the liquid crystalline phases and micelles. KEY WORDS: Microemulsions, SAXS, FRET, Lipolysis, Mucus, Liquid crystalline phase
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spelling doaj.art-2822e3a1edf14ac2b9b533beb6c20db22022-12-22T01:08:17ZengElsevierActa Pharmaceutica Sinica B2211-38352018-07-0184655665In situ monitoring of the structural change of microemulsions in simulated gastrointestinal conditions by SAXS and FRETXia Lv0Shuguang Zhang1Huipeng Ma2Peipei Dong3Xiaodong Ma4Ming Xu5Yan Tian6Zeyao Tang7Jinyong Peng8Haibo Chen9Jianbin Zhang10College of Pharmacy, Dalian Medical University, Dalian 116044, China; College of Life Science, Dalian Minzu University, Dalian 116600, ChinaXinglin College, Liaoning University of Traditional Chinese Medicine, Shenyang 110167, ChinaCollege of Medical Laboratory, Dalian Medical University, Dalian 116044, ChinaCollege of Pharmacy, Dalian Medical University, Dalian 116044, ChinaCollege of Pharmacy, Dalian Medical University, Dalian 116044, ChinaCollege of Pharmacy, Dalian Medical University, Dalian 116044, ChinaCollege of Pharmacy, Dalian Medical University, Dalian 116044, ChinaCollege of Pharmacy, Dalian Medical University, Dalian 116044, ChinaCollege of Pharmacy, Dalian Medical University, Dalian 116044, ChinaCollege of Pharmacy, Dalian Medical University, Dalian 116044, ChinaCollege of Pharmacy, Dalian Medical University, Dalian 116044, China; Corresponding author.Microemulsions are promising drug delivery systems for the oral administration of poorly water-soluble drugs. However, the evolution of microemulsions in the gastrointestinal tract is still poorly characterized, especially the structural change of microemulsions under the effect of lipase and mucus. To better understand the fate of microemulsions in the gastrointestinal tract, we applied small-angle X-ray scattering (SAXS) and fluorescence resonance energy transfer (FRET) to monitor the structural change of microemulsions under the effect of lipolysis and mucus. First, the effect of lipolysis on microemulsions was studied by SAXS, which found the generation of liquid crystalline phases. Meanwhile, FRET spectra indicated micelles with smaller particle sizes were generated during lipolysis, which could be affected by CaCl2, bile salts and lecithin. Then, the effect of mucus on the structural change of lipolysed microemulsions was studied. The results of SAXS and FRET indicated that the liquid crystalline phases disappeared, and more micelles were generated. In summary, we studied the structural change of microemulsions in simulated gastrointestinal conditions by SAXS and FRET, and successfully monitored the appearance and disappearance of the liquid crystalline phases and micelles. KEY WORDS: Microemulsions, SAXS, FRET, Lipolysis, Mucus, Liquid crystalline phasehttp://www.sciencedirect.com/science/article/pii/S2211383517306846
spellingShingle Xia Lv
Shuguang Zhang
Huipeng Ma
Peipei Dong
Xiaodong Ma
Ming Xu
Yan Tian
Zeyao Tang
Jinyong Peng
Haibo Chen
Jianbin Zhang
In situ monitoring of the structural change of microemulsions in simulated gastrointestinal conditions by SAXS and FRET
Acta Pharmaceutica Sinica B
title In situ monitoring of the structural change of microemulsions in simulated gastrointestinal conditions by SAXS and FRET
title_full In situ monitoring of the structural change of microemulsions in simulated gastrointestinal conditions by SAXS and FRET
title_fullStr In situ monitoring of the structural change of microemulsions in simulated gastrointestinal conditions by SAXS and FRET
title_full_unstemmed In situ monitoring of the structural change of microemulsions in simulated gastrointestinal conditions by SAXS and FRET
title_short In situ monitoring of the structural change of microemulsions in simulated gastrointestinal conditions by SAXS and FRET
title_sort in situ monitoring of the structural change of microemulsions in simulated gastrointestinal conditions by saxs and fret
url http://www.sciencedirect.com/science/article/pii/S2211383517306846
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