Abstract：
:Porphyrin and their derivatives are being systematically studied as photosensitizers for photodynamic therapy. The ability to predict their membrane partition properties is of key importance to unveil their in vivo activity and applications. Several n-octanol/water partition coefficients (logP(OW)) of porphyrin derivatives have been reported in the literature but large discrepancies have been observed. Reproducible and reliable logP(OW) data for a series of 20 cationic meso-phenyl(pyridyl)porphyrin derivatives were determined by correlating logP(OW) with the partition coefficients measured in a more adequate n-butanol/water system. Linear correlations as a function of the number of positively charged groups bound to the periphery of the porphyrin rings were found within each series. A significant effect of the stereochemistry and nature of the positively charged substituents was also observed, but diminished steadily converging to a similar value in the mono-substituted derivatives. Binding constants to liposomes were shown to be proportional to logP(OW), except for the cis-isomers of doubly charged porphyrins. The cis-isomer presented smaller logP(OW) and higher membrane affinity. The effect was explained based on the amphiphilic nature of the cis-porphyrin.
journal_name
Int J Pharmjournal_title
International journal of pharmaceuticsauthors
Engelmann FM,Rocha SV,Toma HE,Araki K,Baptista MSdoi
10.1016/j.ijpharm.2006.08.008subject
Has Abstractpub_date
2007-02-01 00:00:00pages
12-8issue
1-2eissn
0378-5173issn
1873-3476pii
S0378-5173(06)00659-4journal_volume
329pub_type
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