| | 1 | Author
| IouriE. Borissevitcha+, ChristianeP F Borgesa++, GalinaP. Borissevitcha+++, VictorE. Yushmanova+, SoniaR W Louroh, Marcel Tabaka | Requires cookie* | | | Title
| Binding and Location of Dipyridamole Derivatives in Micelles: the Role of Drug Molecular Structure and Charge  | | | | Abstract
| Binding and localization of the vasodilator and antitumor drug coactivator dipyridamole (D IP) and of its three derivatives, RA14. RA47 and RA25 (D IP D), to cationic (cetyltrimeth-ylammonium chloride), anionic (sodium dodecylsulfate), zwitterionic (N-hexadecyl-N.N-di-methyl-3-ammonio-l-propanesulfonate). and neutral (r-octylphenoxypolyethoxyethanol) m i celles was studied using fluorescence, optical absorption and 'H N M R spectroscopy. The analysis of N M R . optical absorption and fluorescence data indicates that the depth of local ization of the drugs in the micelles from the surface decreased in the order D IP > RA 14 > RA47 > RA25. The binding constants for the neutral drug forms change in the same order in the range of 1400-3100 m _1 for D IP to 80-300 m _1 for RA25. This order is identical with the reported biological activity of D IP D . For the protonated drugs in zwitterionic or neutral micelles the binding constants are reduced by a factor of 20-75. | | | |
Reference
| Z. Naturforsch. 51c, 578—590 (1996); received March 28/May 31 1996 | | | |
Published
| 1996 | | | |
Keywords
| Dipyridamole and Derivatives, Micelle, Drug Location, Absorption, Fluorescence, N M R | | | |
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| default:Reihe_C/51/ZNC-1996-51c-0578.pdf | | | | Identifier
| ZNC-1996-51c-0578 | | | | Volume
| 51 | |
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