Covalent polar lipid conjugates with neurologically active compo

Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Liposomes

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514 2, 514649, 514212, 5142222, 5142235, 5142248, 5142275, A61K 9127, A61K 3800, A61K 31135, A61K 3154

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active

060249773

ABSTRACT:
This invention herein describes a method of facilitating the entry of drugs into cells and tissues at physiologically protected sites at pharmicokinetically useful levels and also a method of targeting drugs to specific organelles within the cell. This polar lipid/drug conjugate targeting invention embodies an advance over other drug targeting methods known in the prior art, because the invention provides drug concentrations in such physiologically protected sites that can reach therapeutically-effective levels after administration of systemic levels much lower than are currently administered to achieve a therapeutic dose. This technology is appropriate for use with psychotropic, neurotropic and neurological drugs, agents and compounds, for rapid and efficient introduction of such agents across the blood-brain barrier. Further, the invention provides means for retention and prolonged enzymatic release of psychotropic, neurotropic and neurological drugs, agents and compounds comprising the conjugates of the invention, in the brain and central nervous system.

REFERENCES:
patent: 4780455 (1988-10-01), Liberman et al.
patent: 4793986 (1988-12-01), Serino et al.
patent: 4847240 (1989-07-01), Ryser et al.
patent: 5017566 (1991-05-01), Bodor
patent: 5023252 (1991-06-01), Hseih
patent: 5024998 (1991-06-01), Bodor
patent: 5039794 (1991-08-01), Wier et al.
patent: 5053394 (1991-10-01), Ellestad et al.
patent: 5112863 (1992-05-01), Hashimoto et al.
patent: 5124146 (1992-06-01), Neuwelt
patent: 5149794 (1992-09-01), Yatvin et al.
patent: 5153179 (1992-10-01), Eibl
patent: 5177064 (1993-01-01), Bodor
patent: 5254342 (1993-10-01), Shen et al.
patent: 5258453 (1993-11-01), Kopecek et al.
patent: 5270312 (1993-12-01), Glase et al.
patent: 5284876 (1994-02-01), Shashoua et al.
patent: 5389623 (1995-02-01), Bodor
patent: 5405834 (1995-04-01), Bundgaard et al.
patent: 5413996 (1995-05-01), Bodor
patent: 5434137 (1995-07-01), Black
patent: 5442043 (1995-08-01), Fukuta et al.
patent: 5466683 (1995-11-01), Sterling et al.
patent: 5525727 (1996-06-01), Bodor
patent: 5543389 (1996-08-01), Yatvin et al.
patent: 5543390 (1996-08-01), Yatvin et al.
Abbas et al., "Antigen Presentation and T Cell Antigen Recognition," Cellular as J. Mol. Immunol. (W.B. Saunders Co.; Philadelphia), pp. 116-136 (1988).
Afzelius et al., Biochim. Biophys. Acta979:231-238 (1989).
Alvarez-Dominquez et al., "Role of Complement Component C1q in Phagocytosis of Listeria monocytogenes by Murine Macrophage-Like Cell Lines," Infect. Immun. 61:3644-3672 (1993).
Anderson et al., J. Am. Chem. Soc. 85: 3039 (1963).
Ashborn et al., Anti-HIV Activity of CD4-Pseudomonas Exotoxin on Infected Primary Human Lymphocytes and Monocyte/Macrophages, J. Infect. Dis. 163: 703-709 (1991).
Baer, Can. J. Biochem. Phys. 34:288-304 (1955).
Bai and Amidon, "Structural Specificity of Mucosal-Cell Transport and Metabolism of Peptide Drugs: Implications for Oral Peptide Drug Delivery," Pharm. Res. 9: 969-978 (1992).
Bai et al., "Utilization of Peptide Carrier System to Improve Intestinal Absorption: Targeting Prolidase as a Prodrug-Converting Enzyme," J. Pharm. Sci. 81: 113-116 (1992).
Barlow et al., "Mast cells and T lymphocytes in chronic urticaria," Clinical & Experimental Allergy 25: 317-322 (1995).
Baroni et al., "Expression of HIV in Lymph Node Cells of LAS Patients: Immunohistology, In Situ Hybridization, and Identification of Target Cells," Am. J. Pathol. 133: 498-506 (1988).
Berdel et al., Lipids 22: 943-946 (1987).
Bickel et al., "Pharmacologic effects in vivo in brain by vector-mediated peptide drug delivery," Proc. Natl. Acad. Sci. USA 90: 2618-2622 (1993).
Blakey, "Drug Targeting with Monoclonal Antibodies," Acta Oncol. 31: 91-97 (1992).
Blight et al., "Detection of hepatitis C virus RNA by in situ hybridization," Liver 12: 286-289 (1992).
Blum et al., "Bloood clearance and organ deposition of intravenously administered colloidal particles: the effects of particle size, nature and shape," Int. J. Pharm. 12: 135-146 (1982).
Boehnlein et al., "Characterization of Esterase and Alcohol Dehydrogenase Activity in Skin. Metabolism of Retinyl Palmitate to Retinol (Vitamin A) During Percutaneous Absorption," Pharmaceutical Research 11: 1155-1159 (1994).
Boman et al., "Cell-free immunity in Cecropia: A model system for antibacterial proteins," Eur. J. Biochem. 201: 23-31 (1990).
Borissova et al., "Biodegradable Microspheres. 17. Lysosomal Degradation of Primaquine-Peptide Spacer Arms," Journal of Pharmaceutical Sciences, vol. 84, No. 2, Feb. 1995, pp. 256-262.
Bou-Gharios et al., "Expression of ectopeptidases in scleroderma," Annals of Rheumatic Disease 54: 111-116 (1995).
Brewster et al., "Improved Delivery through Biological Membranes XXXI: Solubilization and Stabilization of an Estradiol Chemical Delivery System by Modified .beta.-Cyclodextrins," J. Pharm. Sci. 77: 981-985 (1985).
Bromberg et al., "Detection of Borditella pertussis Associated with the Alveolar Macrophages of Children with Human Immunodeficiency Virus Infection," Infect. Immun. 59: 4715-4719 (1991).
Brown & Silvius, Biochim. Biophys. Acta 1023: 341-351 (1990).
Brown et al., "Induction of Cell Surface Peptidase Activity: A Global Response to Cell Stress Correlated with Apoptosis," J. Cellular Biochemistry 54: 320-331 (1994).
Brynestad et al., J. Virol. 64:680-685 (1990).
Buchmeier and Heffron, "Induction of Salmonella Stress Proteins upon Infection of Macrophages," Science 248: 730-732 (1990).
Buyuktimkin et al., "Synthesis and Enhancing Effect of Dodecyl 2-(N,N-Dimethylamino)propionate on the Transepidermal Delivery of Indomethacin, Clondine, and Hydrocotisone," Pharmaceutical Research 10: 1632-1637 (1993).
Chang, "Leishmania donovani: Promastigote-Macrophage Surface Interactions in Vitro," Exp. Parisitol. 48:175-189 (1979).
Clarke et al., "Detection of HIV-1 in human lung macrophages using the polymerase chaine reaction," AIDS 4: 1133-1136 (1990).
Comiskey & Health, Biochim, Biophys. Acta 1024: 307-317 (1990).
Cordier et al., "In vivo Activation of Alveolar Macrophages in Ovine Lentivirus Infection," Clin. Immunol. Immunopathol. 55: 355-367 (1990).
Couveur and Puisieux, "Nano-and microparticles for the delivery of polypeptides and proteins," Adv. Drug Deliv. Rev. 10: 141-162 (1993).
Dachun et al., "Localization and Quantification of the Nonspecific Esterase in Injured Skin for Timing of Wounds," Forensic Science International 53: 202-213 (1992).
De Magistris et al., "Antigen Analog-Major Histocompatibility Complexes Act As Antagonists of the T Cell Receptor," Cell 68: 625-634 (1992).
Debs et al., Biochim. Biophys. Acta 901: 183-190 (1987).
Deres et al., Nature 342:561-564 (1989).
Dreyer et al., Proc. Natl. Acad. Sci. USA 86: 9752-9756 (1989).
Duncan, "Drug-polymer conjugates: potential for improved chemotherapy," Anticancer Drugs 3: 175-210 (1992).
Elliott et al., "Naturally processed peptides," Nature 348: 195-197 (1990).
Embretson et al., "Massive convert infection of helper T lymphocytes and macrophages by HIV during the incubation period of AIDS," Nature 362: 359-361 (1993).
Falk et al., "Allele-specific motifs revealed by sequencing of self-peptides eluted from MHC molecules," Nature 351: 290-291 (1991).
Falk et al., "Cellular peptide composition governed by major histocompatability complex class I molecules," Nature 348: 248-251 (1990).
Faulk et al., "Transferrin-Adriamycin Conjugates which Inhibit Tumor Cell Proliferation without Interaction with DNA Inhibit Plasma Membrane Oxidoreductase and Proton Release in K562 Cells," Biochem. Int. 25: 815-822 (1991).
Faustman et al., "Linkage of Faulty Major Histocompatability Complex Class I to Autoimmune Diabetes," Science 254: 1756-1776 (1991).
Franssen et al., "Low Molecular Weight Proteins as Carrier for Renal Drug Targeting: Preparation of Drug-Protein Conjugates and Drug-Spacer Derivatives and Their Catabolism in Renal Cortex Homogenates and Lysosomal Lysates," J. Med. Chem. 35: 1246-1259 (1992).
Frehel et al., "Intramacrophage Growth of Mycobacterium avium during Infection of Mice," Infect. Immun. 59: 2207-2214 (1991).
Friedman et

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