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J Pharm Sci ; 100(7): 2724-33, 2011 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-21283989

RESUMO

Dendritic cells (DCs) are able to present glycolipids to invariant natural killer T (iNKT) cells in vivo. Very few compounds have been found to stimulate iNKT cells, and of these, the best characterised is the glycolipid α-galactosylceramide, which stimulates the production of large quantities of interferon-gamma (IFN-γ) and interleukin-4 (IL-4). However, αGalCer leads to overstimulation of iNKT cells. It has been demonstrated that the αGalCer analogue, threitol ceramide (ThrCer 2), successfully activates iNKT cells and overcomes the problematic iNKT cell activation-induced anergy. In this study, ThrCer 2 has been inserted into the bilayers of liposomes composed of a neutral lipid, 1,2-distearoyl-sn-glycero-3-phosphocholine (DSPC), or dimethyldioctadecylammonium bromide (DDA), a cationic lipid. Incorporation efficiencies of ThrCer within the liposomes was 96% for DSPC liposomes and 80% for DDA liposomes, with the vesicle size (large multilamellar vs. small unilamellar vesicles) making no significant difference. Langmuir-Blodgett studies suggest that both DSPC and DDA stack within the monolayer co-operatively with the ThrCer molecules with no condensing effect. In terms of cellular responses, IFN-γ secretion was higher for cells treated with small DDA liposomes compared with the other liposome formulations, suggesting that ThrCer encapsulation in this liposome formulation resulted in a higher uptake by DCs.


Assuntos
Adjuvantes Imunológicos/farmacologia , Células Dendríticas/efeitos dos fármacos , Galactosilceramidas/farmacologia , Células Matadoras Naturais/efeitos dos fármacos , Fosfatidilcolinas/química , Compostos de Amônio Quaternário/química , Álcoois Açúcares/farmacologia , Adjuvantes Imunológicos/administração & dosagem , Adjuvantes Imunológicos/química , Células Cultivadas , Química Farmacêutica , Células Dendríticas/imunologia , Composição de Medicamentos , Estabilidade de Medicamentos , Galactosilceramidas/administração & dosagem , Galactosilceramidas/química , Humanos , Interferon gama/metabolismo , Células Matadoras Naturais/imunologia , Cinética , Lipossomos , Tamanho da Partícula , Solubilidade , Álcoois Açúcares/administração & dosagem , Álcoois Açúcares/química , Tecnologia Farmacêutica/métodos
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