Abstract: The present invention relates to formulations of a lipid based controlled-release matrix, a polyhydroxy component and a bioactive agent. Such formulation are useful in the delivery of the bioactive compounds. The invention also relates to the use of a polyhydroxy component for increasing the solubility of a bioactive compound, especially a peptide in a lipid-based controlled-release matrix.

Abstract: 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.

Abstract: The present invention relates to particulate compositions comprising at least 50% of dioleoyl phosphatidyl ethanolamine (DOPE) and 1 to 50% of Polysorbate 80 (P80). All parts are by weight relative to the sum of the weights of a+b and the compositions comprise non-lamellar particles or form non-lamellar particles when contacted with an aqueous fluid. The compositions have advantageous stability and low toxicity and the invention also relates to pharmaceutical compositions thereof.

Abstract: 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 opioid 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.

Abstract: The invention provides a composition suitable for administration to a mammalian, particularly human, subject wherein the composition comprises an active agent and an amphilic component (containing at least one amphiphile) wherein at least a portion of the amphiphilic component is an ether-linked lipid and wherein the composition includes a non-lamellar phase, preferably in the form of particles, or forms a non-lamellar phase on contact with an aqueous liquid. The aqueous liquid may be a body fluid. The invention also provides pharmaceutical and cosmetic formulations comprising the compositions and methods for their formation.

Abstract: The present invention provides a method for the production of amphiphile particles having incorporated therein at least one active agent. The method comprises forming a dispersion of particles comprising at least one amphiphilic structuring agent in a solution of at least one active agent, heating said dispersion to an elevated temperature, followed by cooling to around ambient temperature. The loading provided thereby is typically at least 130% of the loading provided by equilibration of the particles in a solution of active agent. The invention also provides corresponding amphiphile particles.

Abstract: The present invention relates to compositions containing at least one cationic peptide active agent, at least one neutral structure forming amphiphile, at least one anionic structure forming amphiphile and optionally at least one solvent wherein the composition is in the form of a non-lamellar phase structure and/or forms a non-lamellar phase structure on exposure to body fluids. The invention also relates to methods for protecting peptides from enzymic degredation in vivo and to compositions in which the peptide active agent is so protected.