Abstract: siRNA-conjugated liposomes and micelles, methods of making such conjugates, and methods of using such conjugates, such as for the delivery of siRNA to cells to reduce expression of target polypeptides in such cells, are described.

Abstract: What is described are macrocyclic compounds formed by reaction of a cyclic compound, which contains an amine, with an epoxide. The macrocyclic compound has the following structure: When substituents R and R? that are hydrophobic substituents, the macrocyclic compound functions as a lipid and is compatible with lipid systems, including liposomes and lipid particles. When present in certain lipid systems, the macrocyclic compound enhances the ability of the lipid system to facilitate delivery of therapeutic molecules to target cells in a mammalian subject.

Abstract: Compositions comprising a heterogeneous polymeric micelle and an agent (e.g., a polynucleotide) associated with the micelle are disclosed, together with methods for intracellular delivery of such agent.

Abstract: The present invention provides a process for preparing a pharmaceutical composition of fingolimod comprising: (i) obtaining a intimate admixture comprising fingolimod or a pharmaceutically acceptable salt thereof, and at least one surfactant (wetting agent), e.g., an intimate admixture of the fingolimod and the at least one surfactant, and (ii) optionally combining the intimate admixture from step (i) with one or more excipients. Also provided are pharmaceutical compositions and dosage forms obtainable by the process, uses of the pharmaceutical compositions and dosage forms, and methods of treating appropriate diseases with the pharmaceutical compositions or dosage forms.

Abstract: The conjugates of present invention are formed by the combination of rhein or their analogues with the organic bases or amino acids in molecular force between them. The methods for preparing the conjugates and their uses for manufacturing medicines in the treatment of diabetic nephrosis, recovery of gastrointestinal function and prevention of intestinal adhesion, as well as treatment of osteoarthritis, rheumatic arthritis and rheumatoid arthritis are also described. Rhein or their analogues as the left part of general formula (I) is selected from (1) the compounds of rhein or their analogues, in which one or two substituents of R2˜R3 and R6˜R7 are COOH at least two substituents of R1˜8 are —H; or (2) the rhein-containing extract derived from plants. In general formula (I), M represents nitrogen-containing organic bases or basic amino acids.

Abstract: The present application discloses a targeting composition that actively targets chitin-like materials, such as those found in fungi, a drug delivery vehicle comprising a micelle that comprises the targeting composition and one or more anti-fungal drugs, and methods of using the drug delivery vehicle.

Abstract: This invention relates to methods for increasing the efficiency of siRNA administrations via pre-administration of an agent that increases LDL receptor levels.

Abstract: This invention relates to biphasic lipid-vesicle compositions and methods for treating cervical displasia by intravaginal delivery.

Abstract: A method of treating the symptoms of spasticity comprises implanting a reservoir-based drug delivery composition into a subject to systemically deliver a therapeutically effective amount of tizanidine to the subject for a long period of time (e.g., one month or one year). The drug delivery composition may include a rate-controlling excipient (e.g., an elastomeric polymer) defining a reservoir containing at least one discrete solid dosage form (e.g., one or more pellets), which includes tizanidine free base and optionally, a sorption enhancer.

Abstract: Here described are compounds of formula I: wherein R1 and R2 is independently selected from a group consisting of C10 to C18 alkyl, C12 to C18 alkenyl, and oleyl group; wherein R3 and R4 are independently selected from a group consisting of C1 to C6 alkyl, and C2 to C6 alkanol; wherein X is selected from a group consisting of —CH2—, —S—, and —O— or absent; wherein Y is selected from —(CH2)n, —S(CH2)n, —O(CH2)n—, thiophene, —SO2(CH2)n—, and ester, wherein n=1-4; wherein a=1-4; wherein b=1-4; wherein c=1-4; and wherein Z is a counterion; as well as compositions and pharmaceutical formulations including compounds of formula I which are useful for the delivery of therapeutic agents; and methods of using these compositions and formulations.

Abstract: This invention relates to biphasic lipid-vesicle compositions and methods for treating cervical displasia by intravaginal delivery.

Abstract: The present invention relates to respirable dry powders that contain respirable dry particles that comprise about 20%-37.5% (w/w) leucine, about 58.6-about 75% (w/w) calcium lactate, and about 3.9-about 5% (w/w) sodium chloride, and methods for treating a subject using the respirable dry powders.

Abstract: This invention relates to biphasic lipid-vesicle compositions and methods for treating cervical displasia by intravaginal delivery.

Abstract: Disclosed is a dentifrice composition comprising an orally acceptable vehicle, an abrasive particulate and a surfactant system comprising an anionic surfactant comprising a C8-C16 fatty acid glutamate salt and a nonionic surfactant comprising a C8-C16 alkyl glucoside.

Abstract: A method of treating the symptoms of spasticity comprises implanting a reservoir-based drug delivery composition into a subject to systemically deliver a therapeutically effective amount of tizanidine to the subject for a long period of time (e.g., one month or one year). The drug delivery composition may include a rate-controlling excipient (e.g., an elastomeric polymer) defining a reservoir containing at least one discrete solid dosage form (e.g., one or more pellets), which includes tizanidine free base and optionally, a sorption enhancer.

Abstract: Formulation of long-acting and controlled release preparations of 2-[(3-chlorophenyl)amino] phenylacetic acid (23CPPA) are disclosed. Long-acting preparations comprise a slow-release formulation coated onto a pharmaceutical composition containing 23CPPA, protect against gastric irritation, slow 23CPPA absorption, extend release of 23CPPA, protect against excessively high 23CPPA blood concentrations, and prolong maintenance of blood concentrations of 23CPPA after administration. Controlled release formulations comprise (a) a core element which is a compressed tablet containing a therapeutic dose of 23CPPA and an amount of a solubility modulating substance that controls the release of said 23CPPA in order to provide a therapeutic level over a period of about 24 hours; and (b) on the outer surface of the core element, a sufficient amount of an enteric coating that causes the 23CPPA to release at a rate that permits the use of once-a-day dosing to maintain steady state therapeutic levels of 23CPPA.

Abstract: The invention relates to polymer-micelle complex. The polymer-micelle complexes include a positively charged micelle selected from the group consisting of a monomeric quaternary ammonium compound, a monomeric biguanide compound, and mixtures thereof. The positively charged micelle is electrostatically bound to a water-soluble polymer bearing a negative charge. The polymer does not comprise block copolymer, latex particles, polymer nanoparticles, cross-linked polymers, silicone copolymer, fluorosurfactant, or amphoteric copolymer. The compositions do not form a coacervate, and do not form a film when applied to a surface.

Abstract: The application relates to topical formulations comprising a phase II enzyme inducer precursor and an activating agent. Methods for producing and using the topical formulations are also provided.

Abstract: The present invention relates to an enteric tablet with improved bioavailability, which is rapidly disintegrated after reaching the intestine to allow dissolution of the active ingredient, and which characteristically reduces the amount of talc to be used and is free of an alkali component.

Abstract: Disclosed is a pH-sensitive block copolymer that forms polyionic complex micelles. The block copolymer is prepared by copolymerization of (a) a polyethylene glycol compound, (b) a poly(amino acid) compound, and (c) a heterocyclic alkyl amine compound having the ability to induce the formation of ionic complexes. Further disclosed is a drug or protein carrier using the block copolymer.