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The results provide evidence for the involvement of a carrier\u2010mediated mechanism, since the association of HePC at the apical pole of Caco\u20102 cells was (1) saturable as a function of time with a rapid initial incorporation over 5 min followed by a more gradual increase; (2) saturable as a function of concentration over the range studied (2\u2013200 \u03bcM) with a saturable component which followed Michaelis\u2013Menten kinetics (apparent <jats:italic>K<\/jats:italic><jats:sub>m<\/jats:sub> 15.7 \u03bcmol\/L, <jats:italic>V<\/jats:italic><jats:sub>max<\/jats:sub> 39.2 nmol\/mg protein\/h) and a nonspecific diffusion component; (3) partially inhibited by low temperature and ATP depletion, indicating the temperature and energy\u2010dependence of the uptake process. Moreover, we demonstrated, by an albumin back\u2010extraction method, that HePC is internalized via translocation from the outer to the inner leaflet of the plasma membrane and that HePC may preferentially diffuse through intact raft microdomains. In conclusion, our results suggest that incorporation of HePC at the apical membrane of Caco\u20102 cells may occur through a passive diffusion followed by a translocation in the inner membrane leaflet through an active carrier\u2010mediated mechanism.<\/jats:p>","DOI":"10.1007\/s11745-007-3026-8","type":"journal-article","created":{"date-parts":[[2007,2,5]],"date-time":"2007-02-05T07:42:43Z","timestamp":1170661363000},"source":"Crossref","is-referenced-by-count":28,"title":["Inward Translocation of the Phospholipid Analogue Miltefosine across Caco\u20102 Cell Membranes Exhibits Characteristics of a Carrier\u2010mediated Process"],"prefix":"10.1002","volume":"42","author":[{"given":"C\u00e9cile","family":"M\u00e9nez","sequence":"first","affiliation":[{"name":"Laboratoire de Physico\u2010chimie, Pharmacotechnie et Biopharmacie, UMR CNRS 8612 Facult\u00e9 de Pharmacie Univ. Paris\u2010Sud 11 IFR 141, Tour D5, 2\u00e9me \u00e9tage, 5 rue J.B. Cl\u00e9ment Ch\u00e2tenay\u2010Malabry, Cedex 92296 France"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Marion","family":"Buyse","sequence":"additional","affiliation":[{"name":"Laboratoire de Pharmacie Clinique, UPRES 2706 Facult\u00e9 de Pharmacie Univ. Paris\u2010Sud 11 IFR 141 Ch\u00e2tenay\u2010Malabry 92296 France"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Robert","family":"Farinotti","sequence":"additional","affiliation":[{"name":"Laboratoire de Pharmacie Clinique, UPRES 2706 Facult\u00e9 de Pharmacie Univ. Paris\u2010Sud 11 IFR 141 Ch\u00e2tenay\u2010Malabry 92296 France"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Gillian","family":"Barratt","sequence":"additional","affiliation":[{"name":"Laboratoire de Physico\u2010chimie, Pharmacotechnie et Biopharmacie, UMR CNRS 8612 Facult\u00e9 de Pharmacie Univ. Paris\u2010Sud 11 IFR 141, Tour D5, 2\u00e9me \u00e9tage, 5 rue J.B. 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