Aqueous immunologic adjuvant compositions of monophosphoryl...

A - Human Necessities – 61 – K

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A61K 39/39 (2006.01) A61K 9/00 (2006.01) A61P 37/04 (2006.01) A61K 9/127 (2006.01)

Patent

CA 2376829

An aqueous adjuvant composition comprising an attenuated lipid A derivative and a non-immunostimulatory surfactant or surfactants enhances the immunological response in a warm blooded animal to a protein antigen. Attenuated lipid A derivatives useful according to the subject invention include monophosphoryl lipid A and 3-O-deacylated monophosphoryl lipid A. A surfactant or mixtures of surfactants are dissolved in a solvent. 1,2 Dipalmitoyl-sn-glycero-3-phosphocholine is a preferred surfactant. The dissolved surfactant is added to an attenuated lipid A derivative to obtain a mixture. The molar ratio of attenuated lipid A derivative to surfactant in the mixture is about 4:1. The solvent is evaporated and water is added to the resulting film. The suspension is sonicated in a 60 ~C water bath until it becomes clear. Animals administered the adjuvant formulation exhibited increased antibody responses to a given antigen as well as displayed enhanced lymphocyte proliferative and cytotoxic T-lymphocyte responses. Intranasal administration of the aqueous adjuvant composition and an antigen stimulates the production of serum and mucosal secreted IgA.

Une composition adjuvante aqueuse comprenant un dérivé de lipide A atténué et un ou plusieurs tensio-actifs non-immunostimulateurs, augmentent la réponse immunologique à un antigène chez l'animal à sang chaud. Les dérivés de lipide A atténué utiles selon l'invention, comprennent monophosphoryl lipide A et monophosphoryl lipide désacylé en 3-O. Un tensio-actif ou des mélange de tensio-actifs sont dissous dans un solvant. 1,2-dipalmitoyl-sn-glycéro-3-phosphocholine est le tensio-actif préféré. Le tensio-actif dissous est ajouté à un lipide A atténué, de sorte qu'un mélange soit obtenu. Le rapport molaire entre le lipide A atténué et le tensio-actif dans le mélange est d'environ 4 :1. Le solvant est évaporé et de l'eau est ajoutée au film résultant. La suspension est soniquée dans un bain d'eau à 60 ·C jusqu'à ce qu'il devienne transparent. Les animaux auxquel la formule adjuvante a été administrée présentent des réponses anticorps accrues ainsi que des réponses aux lymphocytes prolifératifs et aux lymphocytes T cytotoxiques accrues. L'administration intranasale de la composition adjuvante aqueuse et d'un antigène stimule la production de sérum et d'IgA sécrétée par les muqueuses.

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