title: Trifluoperazine effects on anionic and zwitterionic micelles: a study by small angle X-ray scattering.
abstract: In this work small angle X-ray scattering (SAXS) studies on the interaction of the phenothiazine trifluoperazine (TFP, 2-10 mM), a cationic drug, with micelles of the zwitterionic surfactant 3-(N-hexadecyl-N,N-dimethylammonium) propane sulfonate (HPS, 30 mM) and the anionic surfactant sodium dodecyl sulfate (SDS, 40 mM) at pH 4.0, 7.0, and 9.0 are reported. The data were analyzed through the modeling of the micellar form factor and interference function, as well as by means of the distance distribution function p(r). For anionic micelles (SDS), the results evidence a micellar shape transformation from prolate ellipsoid to cylinder accompanied by micellar growth and surface charge screening as the molar ratio TFP:SDS increases in the complex for all values of pH. Small ellipsoids with axial ratio nu=1.5+/-0.1 (long dimension of 60 A) grow and reassemble into cylinder-like aggregates upon 5 mM drug incorporation (1 TFP:8 SDS monomers) with a decrease of the micelle surface charge. At 10 mM TFP:40 mM SDS cylindrical micelles are totally screened with an axial ratio nu approximately 4 (long dimension approximately 140 A at pH 7.0 and 9.0). However, at pH 4.0, where the drug is partially diprotonated, 10 mM TFP incorporation gives rise to a huge increase in micellar size, resulting in micelles at least 400 A long, without altering the intramicellar core. For zwitterionic micelles (HPS), the results have shown that the aggregates also resemble small prolate ellipsoids with averaged axial ratio approximately nu=1.6+/-0.1. Under TFP addition, both the paraffinic radius and the micellar size show a slight decrease, giving evidence that the micellar hydrophobic core may be affected by phenothiazine incorporation rather than that observed for the SDS/TFP comicelle. Therefore, our results demonstrate that the axial ratio and shape evolution of the surfactant:TFP complex are both dependent on surfactant surface-charge and drug:surfactant molar ratio. The results are compared with those recently obtained for another phenothiazine drug, chlorpromazine (CPZ), in SDS and HPS micelles (Caetano, Gelamo, Tabak, and Itri, J. Colloid Interface Science 248 (2002) 149).
authors.affiliation: Instituto de Física, Universidade de São Paulo, Cx Postal 66318, CEP 05315-970, São Paulo SP, Brazil.
authors.forename: Wilker
authors.initials: W
authors.lastname: Caetano
authors.forename: Leandro R S
authors.initials: LR
authors.lastname: Barbosa
authors.forename: Rosangela
authors.initials: R
authors.lastname: Itri
authors.forename: Marcel
authors.initials: M
authors.lastname: Tabak
mesh_terms: D014150:Antipsychotic Agents / Q000737:chemistry; D008823:Micelles; D012542:Scattering, Radiation; D014268:Trifluoperazine / Q000737:chemistry*; D014965:X-Rays
chemical_list: D014150:Antipsychotic Agents; D008823:Micelles; D014268:Trifluoperazine