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@ARTICLE{PuigRigall:873827,
      author       = {Puig-Rigall, Joan and Fernández-Rubio, Celia and
                      González-Benito, Javier and Houston, Judith E. and
                      Radulescu, Aurel and Nguewa, Paul and González-Gaitano,
                      Gustavo},
      title        = {{S}tructural characterization by scattering and
                      spectroscopic methods and biological evaluation of polymeric
                      micelles of poloxamines and {TPGS} as nanocarriers for
                      miltefosine delivery},
      journal      = {International journal of pharmaceutics},
      volume       = {578},
      issn         = {0378-5173},
      address      = {New York, NY [u.a.]},
      publisher    = {Elsevier},
      reportid     = {FZJ-2020-01031},
      pages        = {119057},
      year         = {2020},
      abstract     = {Miltefosine (MF), an alkylphospholipid originally developed
                      for breast cancer treatment, is a highly active drug for the
                      treatment against leishmaniasis, a neglected tropical
                      disease considered the world’s second leading cause of
                      death by a parasitic agent after malaria. MF exhibits
                      dose-limiting gastrointestinal side effects in patients and
                      its penetration through lipophilic barriers is reduced. In
                      this work we propose a reformulation of MF by incorporating
                      the drug to poly(ethylene)oxide (PEO)-based polymeric
                      micelles, specifically, D-α-tocopheryl polyethylene glycol
                      succinate (TPGS) and Tetronic block copolymers (T904 and
                      T1107). A full structural characterization of the aggregates
                      has been carried out by SANS (small-angle neutron
                      scattering) and dynamic light scattering (DLS), in
                      combination with proton 1D and 2D nuclear magnetic resonance
                      (NMR) spectroscopy, to determine the precise location of the
                      drug. The structure of MF micelles has been characterized as
                      a function of the temperature and concentration. In the
                      presence of the block-copolymers, MF forms mixed micelles in
                      a wide range of temperatures, TPGS being the co-surfactant
                      that incorporates more MF unimers. The hydrophobic tail of
                      MF and those of the block copolymers are in close contact
                      within the micelles, which present a core-shell structure
                      with a hydrophilic corona formed by the PEG blocks of the
                      TPGS and the zwitterion head group of the MF. In order to
                      identify the best carrier, the antileishmanicidal activity
                      of MF in the different formulations has been tested on
                      macrophages, promastigotes and intracellular amastigotes.
                      The combination of the three vehicles with MF makes the
                      formulated drug more active than MF alone against L. major
                      promastigotes, however, only the combination with T904
                      increases the MF activity against intracellular amastigotes.
                      With the aim of exploring gel-based formulations of the
                      drug, the combination of MF and T1107 under gelation
                      conditions has also been investigated.},
      cin          = {JCNS-FRM-II / JCNS-1 / MLZ},
      ddc          = {610},
      cid          = {I:(DE-Juel1)JCNS-FRM-II-20110218 /
                      I:(DE-Juel1)JCNS-1-20110106 / I:(DE-588b)4597118-3},
      pnm          = {6G4 - Jülich Centre for Neutron Research (JCNS) (POF3-623)
                      / 6G15 - FRM II / MLZ (POF3-6G15)},
      pid          = {G:(DE-HGF)POF3-6G4 / G:(DE-HGF)POF3-6G15},
      experiment   = {EXP:(DE-MLZ)KWS2-20140101},
      typ          = {PUB:(DE-HGF)16},
      pubmed       = {pmid:31991188},
      UT           = {WOS:000519297300044},
      doi          = {10.1016/j.ijpharm.2020.119057},
      url          = {https://juser.fz-juelich.de/record/873827},
}