Regulation of Lipid Membrane Partitioning of Tamoxifen by Ionic Strength and Cholesterol
| Autor: | Quan D. Nguyen, Trang T.M. Nguyen, Uyen P.N. Dao |
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| Rok vydání: | 2020 |
| Předmět: |
1
2-Dipalmitoylphosphatidylcholine Pharmaceutical Science 02 engineering and technology 030226 pharmacology & pharmacy Membrane Lipids 03 medical and health sciences chemistry.chemical_compound 0302 clinical medicine stomatognathic system Membrane fluidity Pharmacology (medical) skin and connective tissue diseases Lipid bilayer Pharmacology Liposome Molecular Structure Chemistry Cholesterol Bilayer Cell Membrane Osmolar Concentration Organic Chemistry technology industry and agriculture Phosphatidylglycerols 021001 nanoscience & nanotechnology Tamoxifen Membrane Ionic strength Acyl chain Biophysics Molecular Medicine lipids (amino acids peptides and proteins) 0210 nano-technology hormones hormone substitutes and hormone antagonists Biotechnology |
| Zdroj: | Pharmaceutical Research. 37 |
| ISSN: | 1573-904X 0724-8741 |
| DOI: | 10.1007/s11095-020-2771-8 |
| Popis: | The purpose of this study was to inspect the interactions between an anti-breast cancer, TAM, with model of lipid membranes composed of either zwitterionic DPPC LUVs or anionic DPPG LUVs and how they depend on ionic strength and cholesterol. The Kp of TAM into DPPC and DPPG LUVs were determined at three different NaCl concentrations by second derivative UV-Vis spectrophotometry. The effect of cholesterol incorporated into these LUVs on TAM’s Kp was also assessed. The ATR-FTIR measurements were carried out to verify structural changes within the acyl chain and head group regions of the liposomes upon TAM partitioning. Increasing salt concentration produced negligible impact on the partitioning of TAM into DPPC bilayer as its Kp remained unaffected whilst induced outstanding reduction of TAM’s Kp into DPPG liposomes. Furthermore, TAM was found to disorder the lipids’ acyl chains, which could result in an increase in the membrane fluidity, a necessary piece of information to refer to when prescribing TAM dosage for administration. Additionally, cholesterol showed astoundingly opposite contribution to the partitioning of TAM into the LUVs, as its Kp value reduced in DPPC/Chol bilayer yet increased in DPPG/Chol liposomes. Ionic strength and cholesterol play a noteworthy role in regulation of TAM partitioning into lipid membranes as they could obstruct or promote such action. |
| Databáze: | OpenAIRE |
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