title: Effect of free versus liposomal-complexed pentamidine isethionate on biological characteristics of Acanthamoeba castellanii in vitro.
abstract: Acanthamoeba is an opportunistic protozoan pathogen that can cause blinding keratitis and a rare but fatal encephalitis involving the central nervous system with a very poor prognosis. This is due to limited availability of effective anti-acanthamoebic drugs. Here, we tested whether the use of liposomes can improve the potency of pentamidine isethionate, an anti-amoebic compound. The liposomes consisted of l-alpha-phosphatidylcholine and cholesterol or ergosterol in a molar ratio of 1 : 5. Pentamidine isethionate was incorporated to achieve a final drug to lipid ratio of 1 : 5. At a drug concentration of 10 microg ml(-1), the liposomal drug was >12 times more effective than the free drug at preventing Acanthamoeba binding to human cells and significantly more effective in reducing parasite-mediated human cell cytopathogenicity, compared with the drug alone. Both the free and liposomal drug blocked Acanthamoeba encystation.
authors.affiliation: School of Veterinary Medicine and Science, University of Nottingham, Sutton Bonington LE12 5RD, UK.|School of Biological and Chemical Sciences, Birkbeck College, University of London, London, UK.
authors.forename: Ruqaiyyah
authors.initials: R
authors.lastname: Siddiqui
authors.affiliation: School of Biological and Chemical Sciences, Birkbeck College, University of London, London, UK.
authors.forename: Abdul
authors.initials: A
authors.lastname: Syed
authors.affiliation: School of Biological and Chemical Sciences, Birkbeck College, University of London, London, UK.
authors.forename: Salvador
authors.initials: S
authors.lastname: Tomas
authors.affiliation: School of Pharmacy, University of London, London, UK.
authors.forename: Jose
authors.initials: J
authors.lastname: Prieto-Garcia
authors.affiliation: School of Veterinary Medicine and Science, University of Nottingham, Sutton Bonington LE12 5RD, UK.
authors.forename: Naveed Ahmed
authors.initials: NA
authors.lastname: Khan
mesh_terms: D048248:Acanthamoeba castellanii / Q000187:drug effects* / Q000378:metabolism / Q000472:pathogenicity; D000818:Animals; D000981:Antiprotozoal Agents / Q000008:administration & dosage / Q000494:pharmacology*; D001921:Brain / Q000098:blood supply* / Q000382:microbiology; D002448:Cell Adhesion; D002478:Cells, Cultured; D004730:Endothelium, Vascular / Q000166:cytology* / Q000382:microbiology; D006801:Humans; D008081:Liposomes; D010419:Pentamidine / Q000008:administration & dosage / Q000494:pharmacology*
chemical_list: D000981:Antiprotozoal Agents; D008081:Liposomes; D010419:Pentamidine