Patent classifications
A61K9/1274
CONTROLLED-RELEASE FORMULATIONS
The present invention relates to pre-formulations comprising low viscosity, non-liquid crystalline, mixtures of: a) at least one ester of a sugar or sugar derivative; b) at least one phospholipid; c) at least one biocompatible, oxygen containing, low viscosity organic solvent; wherein the pre-formulation forms, or is capable of forming, at least one liquid crystalline phase structure upon contact with an aqueous fluid; with the proviso that the pre-formulation does not further comprise a liquid crystal hardener. The preformulations are suitable for generating parenteral, non-parenteral and topical depot compositions for sustained release of active agents. The invention additionally relates to a method of delivery of an active agent comprising administration of a preformulation of the invention, a depot composition formed by exposing pre-formulations of the invention to an aqueous fluid, a method of treatment comprising administration of a preformulation of the invention and the use of a preformulation of the invention.
VITAMIN A COMPOSITION
The present invention relates to a composition comprising triglycerides, surfactant, self-assembled structures and vitamin A or provitamin A. Further aspects of the invention are a food product, the use of a composition comprising triglycerides, surfactant and self-assembled structures to stabilize vitamin A or provitamin A and a process for preparing a stabilized vitamin A or provitamin A composition.
LIPID DEPOT FORMULATIONS
The present invention relates to pre-formulations comprising low viscosity, non-liquid crystalline, mixtures of: a) at least one neutral diacyl lipid and/or at least one tocopherol; b) at least one phospholipid; c) at least one biocompatible, oxygen containing, low viscosity organic solvent;
wherein at least one bioactive agent is dissolved or dispersed in the low viscosity mixture and wherein the pre-formulation forms, or is capable of forming, at least one liquid crystalline phase structure upon contact with an aqueous fluid. The preformulations are suitable for generating parenteral, non-parenteral and topical depot compositions for sustained release of active agents. The invention additionally relates to a method of delivery of an active agent comprising administration of a preformulation of the invention, a method of treatment comprising administration of a preformulation of the invention and the use of a preformulation of the invention in a method for the manufacture of a medicament.
TRANSMEMBRANE PORES FORMED BY AROMATIC OLIGOAMIDE FOLDAMERS AND USES OF SAME
Provided are aromatic oligoamide foldamers and self-assembled compositions of the same. The aromatic oligoamide foldamers and compositions can form tube-like structures that can form pores in membranes. The pores can be used to transport ions and molecules, such as, for example, cryoprotective agents or therapeutic agents, through the membrane. The tube-like structures exhibit desirable stability at low temperatures.
COMPOSITIONS AND METHODS OF USE THEREOF FOR TREATMENT OF MASTITIS
Disclosed herein are compositions and methods of use thereof for the treatment of mastitis in dairy cattle. The compositions and methods can have improved effectiveness and duration of activity against mastitis-causing bacteria. In particular embodiments, the methods include treating mastitis infection by intramammary infusion of a disclosed composition.
ORALLY DELIVERED THERAPEUTICAL COMPOSITION AND USE THEREOF
This disclosure is directed to a pharmaceutical composition comprising a bioactive agent (active pharmaceutical ingredient, API) and at least one long chain fatty acid (LCFA), wherein the long chain fatty acid can comprise a carbon chain having at least 10 carbon atoms and can comprise a free carboxylic acid group or a salt thereof. The LCFA-conjugated active pharmaceutical ingredient (API) can be resistant to acid degradation in digestive system and facilitate the delivery of the API across the small intestinal epithelial cell membrane via fatty acid transport protein 4 (FATP4, also known as SLC27A4). The pharmaceutical composition can be formulated in acid-resistant (enteric-release) dosage forms for oral administration in patients. This disclosure is further directed to a process for producing the LCFA-conjugated bioactive agent including protein, polypeptide, small molecule drugs, DNA, RNA, oligonucleotide, or a combination thereof.
Liposomes encapsulating adenosine
Provided are liposomes that encapsulate adenosine. The liposomes may be formed from sphingomyelin or a combination of sphingomyelin and 1,2-dimyristoyl-sn-glycero-3-phosphocholine (DMPC) or a combination of sphingomyelin and 1,2-dimyristoyl-sn-glycero-3-phosphorylglycerol (DMPG) or a combination of sphingomyelin, DMPG, and DMPC. The liposomes encapsulating adenosine may be used to induce cartilage regeneration, treat osteoarthritis, alleviate joint pain, and/or slow, arrest, and/or reverse progressive structural tissue damage associated with osteoarthritis or treat osteoarthritis, rheumatoid arthritis, acute gouty arthritis, and/or synovitis. The liposomes may release adenosine for up to two weeks.
LIQUID CRYSTALLINE STRUCTURE-FORMING OMEGA-3-FATTY ACID COMPOSITION
The present invention relates to a liquid crystalline structure-forming omega-3-fatty acid composition and, more specifically, provides an omega-3-fatty acid composition comprising: amphoteric lipids which form liquid crystalline structures when exposed to aqueous media such as gastrointestinal juice; omega-3 fatty acids or derivatives thereof; and a liquid crystalline structure-forming aid. The omega-3-fatty acid composition forms self-assembled lyotropic liquid crystals which are thermodynamically stable in structure, irrespective of digestion in the gastrointestinal tract, thereby promoting the solubilization and absorption rate of omega-3-fatty acids as well as providing preparations 30% or more smaller in size than conventional soft gel capsules of omega-3-fatty acid preparations. Thus, the composition can be taken with more ease by geriatric patients and the like and allows for provision of omega-3-fatty acid preparations increasing in in-vivo dissolution and absorption.
Polymer nanodiscs for biotechnology and medical applications
The present invention includes compositions, methods, and methods of making and using a nanoscale discoidal membrane comprising: an amphiphilic membrane patch comprising self-assembled molecular amphiphiles capable of supporting one or more membrane proteins in the amphiphilic membrane patch; and one or more amphipathic scaffold macromolecules that encase the nanoscale discoidal membrane.
Depot formulation
A pharmaceutical long acting depot composition is provided as an aid to smoking cessation treatment. The formulation comprises a therapeutically effective amount of varenicline or its pharmaceutically acceptable derivative and pharmaceutically acceptable excipients. The process of preparation of the formulation is also provided.