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 (Author), Shuguang Zhang (Author), Huipeng Ma (Author), Peipei Dong (Author), Xiaodong Ma (Author), Ming Xu (Author), Yan Tian (Author), Zeyao Tang (Author), Jinyong Peng (Author), Haibo Chen (Author), Jianbin Zhang (Author)
Format: Book
Published: Elsevier, 2018-07-01T00:00:00Z.
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042 |a dc 
100 1 0 |a Xia Lv  |e author 
700 1 0 |a Shuguang Zhang  |e author 
700 1 0 |a Huipeng Ma  |e author 
700 1 0 |a Peipei Dong  |e author 
700 1 0 |a Xiaodong Ma  |e author 
700 1 0 |a Ming Xu  |e author 
700 1 0 |a Yan Tian  |e author 
700 1 0 |a Zeyao Tang  |e author 
700 1 0 |a Jinyong Peng  |e author 
700 1 0 |a Haibo Chen  |e author 
700 1 0 |a Jianbin Zhang  |e author 
245 0 0 |a In situ monitoring of the structural change of microemulsions in simulated gastrointestinal conditions by SAXS and FRET 
260 |b Elsevier,   |c 2018-07-01T00:00:00Z. 
500 |a 2211-3835 
500 |a 10.1016/j.apsb.2018.05.008 
520 |a 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 
546 |a EN 
690 |a Therapeutics. Pharmacology 
690 |a RM1-950 
655 7 |a article  |2 local 
786 0 |n Acta Pharmaceutica Sinica B, Vol 8, Iss 4, Pp 655-665 (2018) 
787 0 |n http://www.sciencedirect.com/science/article/pii/S2211383517306846 
787 0 |n https://doaj.org/toc/2211-3835 
856 4 1 |u https://doaj.org/article/2822e3a1edf14ac2b9b533beb6c20db2  |z Connect to this object online.