5th WCSET-2016 at Vietnam 

 

Technical Session - 1

Title:            Interaction of fluoxetine and lipid membranes: effect of cholesterol
Authors:       Nguyen Quan Trinh, Dao Ngoc Phuong Uyen, Nguyen Thao Trang
Abstract:     In this study, the influence of cholesterol on the interaction between fluoxetine, a SSRI antidepressant, and 1, 2-dioleoyl-sn-glycero-3-phosphocholine (DOPC) large unilamellar vesicles (LUVs) was investigated using FTIR to provide insights into the drug’s interaction with lipid membrane. Infrared spectroscopic bands assigned to the CH2 stretching and PO2 - stretching vibrations revealed that fluoxetine at a concentration of 1.14 mM influences both nonpolar and polar parts of DOPC bilayers. The conformational changes, in both phosphate and alkyl chain regions, of the pure DOPC and DOPC containing 10 mol% cholesterol LUVs upon the introduction of fluoxetine were observed. However, with 20 mol% and 28 mol% cholesterol incorporated into the DOPC LUVs, the lipid conformations remain unchanged in the presence of fluoxetine. This suggests that cholesterol at higher concentration, suppresses the partitioning of fluoxetine into DOPC bilayers. These results showed that the interactions of fluoxetine and lipid membrane play a significant role in the drug partitioning and this, in turn, could affect the drug action.

Keywords:  Antidepressant, Fluoxetine, FTIR, Lipid Conformation, Cholesterol
Pages:       044-051

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