The influence of selected steroid hormones on the physicochemical behaviour of DPPC liposomes.
The physicochemical properties of DPPC (1,2-dipalmitoyl-sn-glycero-3-phosphocholine) liposomes used for topical application are pharmaceutically important. Therefore the aim of our study was to establish rapid and efficient methods for the exact characterisation of the physicochemical properties of extruded DPPC liposomes containing low concentration (0.5%, w/w) of different, therapeutically interesting steroid hormones, named 17-beta-estradiol, cpa (cyproterone acetate) and finasteride. In a first step it could be shown that all drugs influenced the liposome size and changed the zeta potential compared to the placebo formulations. Our further analytical strategy was to use micro-calorimetry and ATR-FTIR (Fourier transformed infrared spectroscopy), two powerful and non-destructive methods to confirm the drug incorporation into the liposomes by proving interactions between the phospholipids and the steroids. Thereby it was even possible to localize the location of interaction. The characteristic phase transition temperatures of the phospholipid were decreased by the hormones which was detected by micro-DSC (differential scanning calorimetry). The results of the ATR-FTIR measurements indicated shifts of the specific lipid peaks, the C=O stretching bands and PO(2)(-) antisymmetric double stretching band, in the gel and liquid crystalline phase. A polar as well as a non-polar interaction could be proven. It could be shown that the investigated steroid hormones changed the physical properties of the phospholipid bilayers.
Biruss
Babette
B
Department of Pharmaceutical Technology and Biopharmaceutics, University of Vienna, Althanstrasse 14, 1090 Vienna, Austria.
Dietl
Renate
R
Valenta
Claudia
C
D015060:1,2-Dipalmitoylphosphatidylcholine / Q000737:chemistry*; D002151:Calorimetry; D002244:Carbon / Q000737:chemistry; D017373:Cyproterone Acetate / Q000494:pharmacology*; D004958:Estradiol / Q000494:pharmacology*; D018120:Finasteride / Q000494:pharmacology*; D008051:Lipid Bilayers / Q000737:chemistry*; D008081:Liposomes / Q000737:chemistry*; D010100:Oxygen / Q000737:chemistry; D044367:Phase Transition; D017550:Spectroscopy, Fourier Transform Infrared; D013696:Temperature
D008051:Lipid Bilayers; D008081:Liposomes; D015060:1,2-Dipalmitoylphosphatidylcholine; D017373:Cyproterone Acetate; D004958:Estradiol; D018120:Finasteride; D002244:Carbon; D010100:Oxygen