Organic compounds -- part of the class 532-570 series – Organic compounds – Heavy metal containing
Patent
1993-10-05
1997-03-25
Kelly, Cynthia Harris
Organic compounds -- part of the class 532-570 series
Organic compounds
Heavy metal containing
556138, C07F 1500, C07F 1502
Patent
active
056146523
DESCRIPTION:
BRIEF SUMMARY
This invention relates to the use of particulate agents in therapeutic or prophylactic treatments of conditions involving cellular infection or malfunction.
Many human and animal diseases involve infection or malfunction of the body's cells, eg. by virtue of viral, bacterial (eg. mycobacterial) or protozoal infection or cancerous malfunction. While the body's immune system is generally able to cope with foreign matter, it is not always able to recognise and destroy cells which have become infected or have begun to malfunction. This is particularly serious in the case of certain infections where the pathogen may remain dormant within infected cells for prolonged periods and also where, as for instance is the case with HIV infection, by infecting cells of the immune system the disease weakens the body's ability to defend itself.
Besides vital infection where the parasite is obliged to replicate within a host cell, the range of known intracellular pathogens is wide and includes the pathogens associated with tuberculosis, listeria, Crohn's disease and leprosy as well as brucella, rickettsias and legionella.
Much of the research effort directed at the development of therapeutic agents for the treatment of such diseases has been directed towards the production of complex organic chemicals which on the whole are not very efficiently delivered into the infected or at-risk cells.
The present invention is based on the realisation that effective delivery of inorganic active agents may be achieved by administration of particulate agents incorporating the active inorganic agent where the particles are of a size that permits their endocytosis, or more especially phagocytosis. This administration route is especially attractive since, unlike complex and chemically more delicate organic drugs, inorganic agents and in particular metal cations and radionuclides will generally not be particularly susceptible to loss of activity as a result of exposure to the relatively harsh chemical environments commonly experienced during or following endocytotic particle uptake.
Thus viewed from one aspect the invention provides the use of a physiologically tolerable, preferably inorganic, material containing atoms or ions of a therapeutically or prophylactically effective element for the manufacture of a particulate agent containing said element, said agent being for use in a therapeutic or prophylactic treatment of the human or animal body which involves delivery of said particles or fragments thereof into cells of said body by endocytosis.
Viewed from a further aspect the invention provides a method of prophylactic or therapeutic treatment of the human or animal, preferably mammalian, body said method comprising administering into said body a particulate agent comprising particles of a physiologically tolerable, preferably inorganic, material containing atoms or ions of a therapeutically or prophylactically effective element whereby to deliver said particles or fragments thereof into cells within said body by endocytosis.
Viewed from a still further aspect, the invention provides a pharmaceutical composition comprising endocytosable particles of a physiologically tolerable, preferably inorganic, material containing atoms or ions of a therapeutically or prophylactically effective element together with at least one pharmaceutical carrier or excipient.
In order that delivery of the "active" element into body cells by endocytosis may be achieved, the particles which effectively serve as a carrier for the active element will generally be substantially insoluble in the body fluids that they are to encounter between administration into the body and endocytosis by the targeted cells. Some diminution in particle size can be tolerated of course and if desired particles may of course be provided with protective coatings or disintegrants so as to ensure that particles of desired sizes are present at or throughout the body zone at which endocytotic uptake is desired or so as to ensure that endocytosable particles are present at such sites for a prol
REFERENCES:
patent: 4101435 (1978-07-01), Hasegawa et al.
patent: 5001014 (1991-03-01), Charles et al.
Speiser, Peter P. (1991) "Nanoparticles and Liposomes: A State of the Art" Methods and Findings in Experimental and Clinical Pharmacology 13(5):337-342.
Toshiba Glass Co., Ltd. (1989) Patent Abstracts of Japan 13(496):127 E 843, Abstract No. 1-200605.
Filler Aaron G.
Lever Andrew M.
Harris Kelly Cynthia
Syngenix Limited
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