18102results about How to "Improve bioavailability" patented technology

Auristatin peptides, including MeVal-Val-Dil-Dap-Norephedrine (MMAE) and MeVal-Val-Dil-Dap-Phe (MMAF), were prepared and attached to Ligands through various linkers, including maleimidocaproyl-val-cit-PAB. The resulting ligand drug conjugates were active in vitro and in vivo.

The present invention concerns methods and reagents useful in modulating gene expression in a variety of applications, including use in therapeutic, diagnostic, target validation, and genomic discovery applications. Specifically, the invention relates to synthetic chemically modified small nucleic acid molecules, such as short interfering nucleic acid (siNA), short interfering RNA (siRNA), double-stranded RNA (dsRNA), micro-RNA (miRNA), and short hairpin RNA (shRNA) molecules capable of mediating RNA interference (RNAi) against target nucleic acid sequences. The small nucleic acid molecules are useful in the treatment of any disease or condition that responds to modulation of gene expression or activity in a cell, tissue, or organism.

The present invention provides solid pharmaceutical compositions for improved delivery of a wide variety of pharmaceutical active ingredients contained therein or separately administered. In one embodiment, the solid pharmaceutical composition includes a solid carrier, the solid carrier including a substrate and an encapsulation coat on the substrate. The encapsulation coat can include different combinations of pharmaceutical active ingredients, hydrophilic surfactant, lipophilic surfactants and triglycerides. In another embodiment, the solid pharmaceutical composition includes a solid carrier, the solid carrier being formed of different combinations of pharmaceutical active ingredients, hydrophilic surfactants, lipophilic surfactants and triglycerides. The compositions of the present invention can be used for improved delivery of hydrophilic or hydrophobic pharmaceutical active ingredients, such as drugs, nutritional agents, cosmeceuticals and diagnostic agents.

A method for preparing a protein or peptide powder is provided that includes spray drying a solution including more than, e.g., about 50 mg/mL of a protein or peptide (e.g., an antibody or antigen binding portion thereof), and at least one excipient. Also provided are stable powdered compositions including a protein and an excipient having less than, e.g., about 6% residual moisture.

The present invention relates to a therapeutic polypeptide and methods for its creation and use for modulating an immune response in a host organism in need thereof. In particular, the invention relates to the administration to an organism in need thereof, of an effective amount of a pre-coupled polypeptide complex comprising a lymphokine polypeptide portion, for example IL-15 (SEQ ID NO: 5, 6), IL-2 (SEQ ID NO: 10, 12) or combinations of both, and an interleukin receptor polypeptide portion, for example IL-15Ra (SEQ ID NO: 7, 8), IL-2Ra (SEQ ID NO: 9, 11) or combinations of both, for augmenting the immune system in, for example, cancer, SCID, AIDS, or vaccination; or inhibiting the immune system in, for example, rheumatoid arthritis, or Lupus. The therapeutic complex of the invention surprisingly demonstrates increased half-life, and efficacy in vivo.

Methods of treating a refractory or drug resistant cancer, cell proliferative disorder and tumor cells are provided. Also provided are antibody drug conjugate metabolites.

The invention concerns a method for the targeted selection of a double-stranded ribonucleic acid (dsRNA) consisting of two single strands that exhibits increased effectiveness in inhibiting the expression of a target gene by means of RNA interference, whereby the sequences of the single strands of the dsRNA are selected in such a way that on both ends of the dsRNA the last complementary nucleotide pair is a G-C, or at least two of the last four complementary nucleotide pairs are G-C pairs; whereby the dsRNA exhibits a single-stranded overhang consisting of 1 to 4 unpaired nucleotides at the first end, and no overhang at the second end; whereby the unpaired nucleotide of the single-stranded overhang that is directly adjacent to the last complementary nucleotide pair contains a purine base.

Disclosed is the use of a mist of a pharmaceutical composition for ophthalmic delivery of a protein or peptide active pharmaceutical ingredient, a related method of treatment and a device useful in implementing the use and method. Disclosed is also the use of a mist for ophthalmic delivery of a pharmaceutical composition including a highly irritating penetration enhancer and an ophthalmically acceptable carrier, a related method of treatment and a device useful in implementing the use and method. Disclosed is also a device for ophthalmic administration configured to direct a mist of a pharmaceutical composition to the eye only when the eye is open. Disclosed is also a self-sterilizing device for ophthalmic administration. Disclosed is also a device and a method for increasing the bioavailability of an ophthalmically administered API in a pharmaceutical composition.

A solid state water soluble formulation in granular or tablet form is provided. The formulation is a natural products formulation containing a green tea plant extract in combination with other ingredients which create an effervescent liquid composition upon dispensing the formulation in a liquid. The liquid form of administration, as well as the effervescent properties of the dissolved formulation increase bioavailability of the advantageous components of the green tea plants such as Polyphenols, by increasing absorption speed and amount in the human body. The formulation may include additional components such as, other plant extracts, vitamins, ionic minerals, and other substances purported to be of a health benefit.

The present disclosure relates to novel sustained-release intraocular drug delivery systems and improvements in the treatment of retinopathies. In particular, fibronectin scaffold domain proteins that selectively inhibit VEGFR-2 are contemplated.

Compositions are provided comprising a lipophilic active compound, e.g., a human or veterinary drug or a nutraceutical, interwoven with a polymeric matrix formed by two or more polymers, wherein one of the polymers is an amphiphilic polymer and the other polymer is either an amphiphilic polymer with a different hydrophobic-hydrophilic balance or a hydrophilic polymer, and the active lipophilic compound has modified physicochemical properties. The composition forms colloidal nanodispersion upon contact with aqueous media.

Drugs, especially low aqueous solubility drugs, are provided in a porous matrix form, preferably microparticles, which enhances dissolution of the drug in aqueous media. The drug matrices preferably are made using a process that includes (i) dissolving a drug, preferably a drug having low aqueous solubility, in a volatile solvent to form a drug solution, (ii) combining at least one pore forming agent with the drug solution to form an emulsion, suspension, or second solution and hydrophilic or hydrophobic excipients that stabilize the drug and inhibit crystallization, and (iii) removing the volatile solvent and pore forming agent from the emulsion, suspension, or second solution to yield the porous matrix of drug. Hydrophobic or hydrophilic excipients may be selected to stabilize the drug in crystalline form by inhibiting crystal growth or to stabilize the drug in amorphous form by preventing crystallization. The pore forming agent can be either a volatile liquid that is immiscible with the drug solvent or a volatile solid-compound, preferably a volatile salt. In a preferred embodiment, spray drying is used to remove the solvents and the pore forming agent. The resulting porous matrix has a faster rate of dissolution following administration to a patient, as compared to non-porous matrix forms of the drug. In a preferred embodiment, microparticles of the porous drug matrix are reconstituted with an aqueous medium and administered parenterally, or processed using standard techniques into tablets or capsules for oral administration.