Delivery of amphotericin B nanosuspensions to the brain and determination of activity against Balamuthia mandrillaris amebas.
Amphotericin B was formulated as nanosuspensions to develop a nanoparticulate brain delivery system. Nanosuspensions were produced with different surfactant solutions by high-pressure homogenization and then characterized by laser diffractometry and photon correlation spectroscopy. Before in vitro and in vivo testing all nanosuspensions were investigated for protein adsorption by two-dimensional polyacrylamide gel electrophoresis to predict brain-targeting capacities. Selected nanosuspensions were tested for amebicidal activity against Balamuthia mandrillaris, an agent of lethal encephalitis. Our results indicate that nanosuspensions coated with polysorbate 80 and sodium cholate markedly increased drug brain delivery and inhibited the parasite in vitro, though less in vivo. From the clinical editor: The antifungal Amphotericin B was formulated as nanosuspensions to develop a nanoparticulate brain delivery system. The results indicate that nanosuspensions coated with polysorbate 80 and sodium cholate markedly increased drug brain delivery and inhibited the parasite in vitro, though less in vivo.
Lemke
Andreas
A
Rijksuniversiteit Groningen, GUIDE, Farmaceutische Biologie, Groningen, The Netherlands.
Kiderlen
Albrecht F
AF
Petri
Boris
B
Kayser
Oliver
O
D000562:Amebiasis / Q000469:parasitology; D000563:Amebicides / Q000008:administration & dosage* / Q000737:chemistry / Q000494:pharmacology; D056894:Amoebozoa / Q000187:drug effects* / Q000378:metabolism; D000666:Amphotericin B / Q000008:administration & dosage* / Q000737:chemistry / Q000494:pharmacology; D000818:Animals; D001921:Brain / Q000187:drug effects / Q000469:parasitology*; D016503:Drug Delivery Systems / Q000379:methods*; D005260:Female; D051379:Mice; D008810:Mice, Inbred C57BL; D049329:Nanostructures / Q000737:chemistry*; D011136:Polysorbates / Q000737:chemistry
D000563:Amebicides; D011136:Polysorbates; D000666:Amphotericin B