Abstract: Methods for validating the in vivo targeting specificity of compounds according to pharmacokinetic criteria are described. An improved method to generate a library of peptides with reduced complexity and enhanced candidate compound membership comprises expressing oligonucleotides encoding cyclic peptides with randomized coding sequences representing the non-bridging amino acids. Also described is determination of structure activity relationships using kinetic technique using in vivo panning. Design of targeting compounds with appropriate space/charge/hydrophobicity conformations can be based on the results of these kinetic structure activity relationship (kSAR) determinations. In addition, compositions resulting from this methodology are useful in treating neuroinflammatory and lung disorders, and disorders involving disseminated blood cell coagulopathy interactions with vascular endothelium.

Abstract: Novel compositions are disclosed which can induce or enhance an immune response against foreign or self antigens (microbial or parasitic) or modulate (that can lead to suppression) the activity of pathogenic cells in inflammatory or autoimmune diseases. Compositions and methods are taught in how to limit the generation of an immune response against formulated peptides and proteins with application in antibody therapy or hormone replacement therapy. Methods of suppressing autoimmunity are also disclosed which use ligands for cellular receptors expressed on cells of the innate immune system and more specifically for down-regulation of autoimmune processes by either deletion or induction of anergy at the level of autoreactive T cells or by triggering active-suppressor T cells that down-regulate the activity of pathogenic cells.

Abstract: In accordance with the present invention there are provided novel Spray-Dried Lipid Microparticles (SDLM) that are comprised of lipid, a ligand and agent. The ligand is specific for a cell surface receptor, thereby enabling targeting of the agent to cells bearing receptors specific for the targeting ligand. In invention embodiments wherein the receptor internalizes upon ligand binding, there are provided compositions and methods for the introduction of agent into specifically targeted cells. In a particular embodiment, the ligand is specific for antigen presenting cells (APC) and the agent is a defined antigen. In this manner, immune responses can be induced against specific antigens, including those which are normally not very antigenic due to the fact that they are inefficiently internalized by APC.