Abstract: The present invention relates to platinum complex chemotherapeutic compounds having the generic structure: wherein n is 0 or 1 and, preferably, one of R1, R2, R3 or R8 is a -(linker)-polymer group that may contain up to four additional platinum chelates.

Abstract: Stable, viscous, mucoadhesive aqueous compositions which are useful for the prevention and treatment of ulcerative, inflammatory, and/or erosive disorders of mucous membranes and/or the delivery of pharmaceutically active compounds to mucosal surfaces for topical treatment or transfer to the systemic circulation.

Abstract: Stable, viscous, mucoadhesive aqueous compositions which are useful for the prevention and treatment of ulcerative, inflammatory, and/or erosive disorders of mucous membranes, especially mucositis.

Abstract: The present invention relates to amidomalonate O,O?—Pt and N,O—Pt chelates and methods of preparing them in essentially pure form.

Abstract: A thin, flexible, bilayer or multi-layer film which when applied to a moist surface of a body tissue adheres and delivers an active agent, pharmaceutical compound, nutraceutical, flavor or other substance to the underlying surface and/or body cavity and erodes at a predetermined rate. In one application, the amount of time that the active agent remains in contact with the teeth surfaces is controlled by the composition and thickness of the backing layer of the composite film. This erosion or residence time can be regulated from one half hour to several hours, depending upon the desired therapeutic or cosmetic application.

Abstract: The present invention relates to purified platinum complexes in which platinum is coordinated to form a single N,O- or O,O-chelate of an amidomalonate. The chelates, and pharmaceutically acceptable formulations thereof, are useful for the treatment of cancer. The platinum chelates may additionally be linked to one or more functional groups which increases water solubility and/or assists in tumor targeting of the chelate. Examples of tumor targeting moieties include polymers, in which one or more platinum chelates are attached to the polymer backbone via linkers capable of being cleaved in the body, and molecules with a high affinity for receptors which are concentrated or upregulated in tumor tissue and/or the tumor vasculature.

Abstract: The present invention relates to a layered pharmaceutical delivery device for the administration of pharmaceuticals or other active compounds to mucosal surfaces. The device may also be used by itself without the incorporation of a therapeutic. The device of the present invention consists of a water-soluble adhesive layer, a non-adhesive, bioerodable backing layer and one or more pharmaceuticals if desired in either or both layers. Upon application, the device adheres to the mucosal surface, providing protection to the treatment site and localized drug delivery. The “Residence Time”, the length of time the device remains on the mucosal surface before complete erosion, can be easily regulated by modifications of the backing layer.

Abstract: Stable, viscous, mucoadhesive aqueous compositions which are useful for the prevention and treatment of ulcerative, inflammatory, and/or erosive disorders of mucous membranes, especially mucositis.

Abstract: Biodegradable cross-linkers are provided having a polyacid core with at least two acidic groups covalently connected to reactive groups usable to cross-link polymer filaments. Between at least one reactive group and an acidic group of the polyacid is a biodegradable region which preferably consists of a hydroxyalkyl acid ester sequence having 1, 2, 3, 4, 5 or 6 hydroxyalkyl acid ester groups. The polyacid may be attached to a water soluble region that is attached to the biodegradable region having attached reactive groups. The hydroxyalkyl acid ester group is preferably a lactate or glycolate. Polyacids include diacids, triacids, tetraacids and pentaacids, and the reactive group may contain a carbon-carbon double bond. A network of cross-linked polymer filaments having adefined biodegradation rate can be formed using the cross-linkers. The network may contain biologically active molecules, and can be in the form of a microparticle or nanoparticle, or hydrogel.

Abstract: The present invention relates to purified platinum complexes in which platinum is coordinated to form a single N,O- or O,O-chelate of an amidomalonate. The chelates, and pharmaceutically acceptable formulations thereof, are useful for the treatment of cancer. The platinum chelates may additionally be linked to one or more functional groups which increases water solubility and/or assists in tumor targeting of the chelate. Examples of tumor targeting moieties include polymers, in which one or more platinum chelates are attached to the polymer backbone via linkers capable of being cleaved in the body, and molecules with a high affinity for receptors which are concentrated or upregulated in tumor tissue and/or the tumor vasculature.

Abstract: A drug carrier composition comprising a drug complexed with dermatan sulfate is disclosed. The drug is preferably an anti tumor drug and may be taxol, a peptide onco-agent or vincristine. The most preferred antitumor drug is doxorubicin. The dermatan sulfate is essentially purified dermatan sulfate with a sulfur content of up to 9% (w/w) and with selective oligosaccharide oversulfation.

Abstract: A polymer-platinum compound for use in tumor treatment is described. The compound is composed of a biodegradable diamido-diamine polymer linked to a platinum species. The platinum species is released from the polymer to yield a platinum species having anti-tumor activity.

Abstract: A polymer-platinum compound for use in tumor treatment is described. The compound is composed of a polymer backbone having platinum-containing side chains spaced along the polymer backbone. The side chains are composed of an oligopeptide attached at one end to the backbone and at the other end to the platinum compound.

Abstract: A method of delivering a therapeutic compound to an in vivo target site having a selected pH, temperature, ligand concentration or binding-molecule characteristic. The method includes entrapping the therapeutic compound in an encapsulated microparticle composition that, when exposed to a selected target stimulus related to pH, temperature, radiation, or the presence of a selected ligand or ion-channel activator, decondenses to release compound into the target site. The encapsulated microparticle composition consists of a condensed-phase particle matrix containing the compound to be delivered in entrapped form, and a stimulus-responsive lipid bilayer membrane formed around the matrix. Localized perturbation of the lipid membrane, and influx of monovalent counterions into the polymer matrix, in response to the selected target stimulus, causes matrix swelling and compound release from the particles.

Abstract: A microparticle composition for use in compound delivery, when the composition is exposed to a selected target stimulus related to pH, temperature, radiation, or the presence of a selected ligand or ion-channel activator, is disclosed. The composition includes a condensed-phase particle matrix containing the compound to be delivered in entrapped form, and a stimulus-responsive lipid bilayer membrane formed around the matrix. Localized perturbation of the lipid membrane, and influx of monovalent counterions into the polymer matrix, in response to the selected target stimulus, causes matrix swelling and compound release from the particles.

Abstract: This application concerns novel agents comprising cationic or chemically basic metal chelators in association with hydrophilic carriers of anionic or chemically acidic saccharides, sulfatoids and glycosaminoglycans. In certain embodiments, the agents comprise metals and metal ions. Covalent and non-covalent chemical and physical means are described for stabilizing the binding of the metal chelators to the carriers. Novel non-covalently bound compositions are described which give uniquely high payloads and ratio of metal chelator to carrier, ranging from a low of about 15% metal chelator by weight, to a characteristic range of 70% to 90% metal chelator by weight.

Abstract: This application concerns novel agents comprising cationic or chemically basic metal chelators in association with hydrophilic carriers of anionic or chemically acidic saccharides, sulfatoids and glycosaminoglycans. In certain embodiments, the agents comprise metals and metal ions. Covalent and non-covalent chemical and physical means are described for stabilizing the binding of the metal chelators to the carriers. Novel non-covalently bound compositions are described which give uniquely high payloads and ratio of metal chelator to carrier, ranging from a low of about 15% metal chelator by weight, to a characteristic range of 70% to 90% metal chelator by weight.

Abstract: The present invention includes an image-enhancing agent comprising a biodegradable, water-soluble polymer, synthetic or naturally derived and having repeating hydrophilic monomeric units with amino or hydroxyl groups. This agent also includes chelating agents comprising functional groups bound to an amino or hydroxyl group of the monomeric units. These chelating agents have a formation constant for divalent or trivalent metal cations of at least about 10.sup.8 at physiological temperature and pH. This image-enhancing agent is biodegradable to intermediary metabolites, excretable chelates, oligomers, monomers or combinations thereof of low toxicity. These image-enhancing agents may further comprise a paramagnetic metal ion for enhancement of the image arising from induced magnetic resonance signals. Images resulting from scanning of gamma particle emissions may be enhanced when the image-enhancing agent of the present invention comprises radioisotopic metal ions emitting gamma particles.

Abstract: The present invention includes an image-enhancing agent comprising a biodegradable, water-soluble polymer, synthetic or naturally derived and having repeating hydrophilic monomeric units with amino or hydroxyl groups. This agent also includes chelating agents comprising functional groups bound to an amino or bydroxyl group of the monomeric units. These chelating agents have a formation constant for divalent or trivalent metal cations of at least about 10.sup.8 at physiological temperature and pH. This image-enhancing agent is biodegradable to intermediary metabolites, excretable chelates, oligomers, monomers or combinations thereof of low toxicity.These image-enhancing agents may further comprise a paramagnetic metal ion for enhancement of the image arising from induced magnetic resonance signals.Images resulting from scanning of gamma particle emissions may be enhanced when the image-enhancing agent of the present invention comprise radioisotopic metal ions emitting gamma particles.