Abstract: The invention provides a composition for delivery of an active agent comprising a plurality of lamellar particles of a biodegradable polymer which is at least in part crystalline, and an active agent adsorbed to at least most of the particles. Preferably the biodegradablepolymer is at least 5% by weight crystalline. Preferred biodegradable polymers are poly(L-lactide) (L.PLA) or copolymers or blends of L.PLA. The particles are especially useful for the immobilization of antigens or allergens for vaccines.

Abstract: The present invention provides a nasal drug delivery composition comprising nicotine or a pharmacologically-acceptable salt or derivative thereof wherein the composition is adapted to delivery a pulse of nicotine for rapid absorption and a controlled release of nicotine for subsequent sustained absorption. The controlled release phase can be achieved by providing an ion-exchange material which will form a complex with the nicotine. The ion-exchange material may be a polymeric material such as a polysaccharide, or may be in the form of bioadhesive ion-exchange microspheres. The pulse release can be achieved by overloading the ion-exchange material with nicotine so that the composition contains some excess nicotine for immediate release and absorption. Alternatively, some nicotine may be associated with a non ion-exchange material which will release the nicotine immediately on contact with the nasal mucosa, for example non-ion-exchange bioadhesive microspheres.

Abstract: A composition for delivering an active agent to the lymphatic system comprises a plurality of colloidal particles and an active agent associated with each particle, wherein the surface of each particle has a hudrophobicity ratio as defined of less than 10, or wherein a modifying agent is adsorbed onto the surface of each particle such that the modifying agent gives an advancing contact angle as defined of less than 60.degree. or wherein the adsorbed layer thickness as defined is less than 10 nm or the albumin uptake ratio is between 0.2 and 0.5. The composition may satisfy one or more of these requirements. Preferred modifying agents are non-ionic surfactants, in particular block copolymers containing polyethyleneglycol.

Abstract: Provided are biodegradable microparticles, which exhibit a linear release profile of active agent, and methods for making the microparticles. The microparticles include a mixture of a biodegradable polymer, a water soluble polymer, and an active agent. Preferred biodegradable polymers include lactide homopolymers or copolymers of lactide and glycolide, and preferred water soluble polymers include poly(ethylene glycol) (PEG) or PEG copolymers. The microparticles are made using an emulsion/solvent extraction method, in which the continuous phase of the secondary emulsion contains an organic solvent that is miscible with the organic solvent in the primary emulsion.

Abstract: A drug delivery system including a plurality of microsphere particles containing an active drug and including a material associated with each particle which material has the property of increasing the bioavailability of the active drug.

Abstract: A drug delivery composition for administration to mucosa is provided. The composition includes a pharmacologically active compound and particles, preferably powder or microspheres, of chitosan or a chitosan derivative or salt wherein the particles are either solidified or partially cross-linked such that they have a zeta potential of +0.5 to +50 mV. Solidified particles are made by treating particles made from a water soluble chitosan salt with an alkaline agent such as sodium hydroxide in a non-acid containing water to render them insoluble.

Abstract: A drug delivery composition for intranasal delivery comprises a plurality of bioadhesive microspheres and active drug associated with each microsphere, at least 90 wt % of the microspheres having a diameter in the range 0.1 .mu.m to 10 .mu.m. The microspheres may be of starch, gelatin, dextran, collagen or albumin. Suitable drugs include peptides, such as insulin, and antigenic vaccine ingredients. The composition may additionally comprise an absorption enhancer. The microspheres are administered to the nasal cavity by a means such that the product of the square of the microsphere diameter and the flow rate is greater than 2000 .mu.m.sup.2.liters/min.

Abstract: A composition for delivering an active agent to the lymphatic system comprises a plurality of colloidal particles and an active agent associated with each particle, wherein the surface of each particle has a hydrophobicity ratio of less than 10 as defined by hydrophobic interaction chromatography.

Abstract: Compositions for delivery of pharmacologically active agents and methods for their administration are provided. In one embodiment, the compositions include a complex of a polycationic polymer and a pharmacologically active agent in a pharmaceutically acceptable carrier. The compositions in one embodiment permit transport of pharmacologically active compounds across mucosal membranes for systemic delivery. The polycationic polymer may be, for example, a polycationic carbohydrate such as a chitosan or a chitosan salt or derivative. The therapeutic agent a preferred embodiment is a vaccine or a nucleic acid, such as a gene or antisense oligonucleotide. The composition may be provided in different forms such as a solution, dispersion, powder or in the form of microspheres.

Abstract: Compositions for trans-mucosal delivery, e.g. intranasal, include a lysophosphatidyl-glycerol compound as the adsorption enhancer. The preferred compounds for delivery are insulin and calcitonin.

Abstract: A drug delivery composition for intranasal delivery comprises a plurality of bioadhesive microspheres and active drug associated with each microsphere, at least 90 wt % of the microspheres having a diameter in the range 0.1 .mu.m to 10 .mu.m. The microspheres may be of starch, gelatin, dextran, collagen or albumin. Suitable drags include peptides, such as insulin, and antigenic vaccine ingredients. The composition may additionally comprise an absorption enhancer. The microspheres are administered m the nasal cavity by a means such that the product of the square of the microsphere diameter and the flow rate is greater than 2000 .mu.m.sup.2.liters/min.

Abstract: A drug delivery system including a plurality of microsphere particles containing an active drug and including a material associated with each particle which material has the property of increasing the bioavailability of the active drug.

Abstract: Hollow microcapsules or solid microspheres for use in diagnostic procedures, as well as methods for making the microcapsules, are provided, which are formed by combining a volatile oil with an aqueous phase including a water soluble material such as a starch, modified starch or proteinaceous material, or a polyethylene glycol (PEG) conjugate, to form a primary emulsion. The primary emulsion then is combined with a second oil, to form a secondary emulsion, and the material is permitted to harden and to form microcapsules around a liquid core of the volatile oil. At least part of the volatile oil then may be removed by evaporation to produce hollow microcapsules. Optionally, all of the volatile oil may be removed prior to hardening of the material, which produces solid microspheres. The The microcapsules can be used in a variety of applications for diagnostic purposes and for drug delivery.

Abstract: A composition for nasal administration of polar metabolites of opioid analgesics comprises a polar metabolite of an opioid analgesic and an absorption promoting agent. Preferred metabolites morphine-6-glucuronide and morphine-6-sulphate. A preferred absorption promoting agent is chitosan but other suitable agents include cationic polymers, bioadhesive agents, surface active agents, fatty acids, chelating agents, mucolytic agents, cyclodextrin, microsphere preparations or combinations thereof.

Abstract: A composition for administration to the mucosa comprises a pharmacologically active compound and a polycationic substance. The polycationic substance is preferably DEAE-dextran or chitosan and the pharmacologically active compound is preferably insulin or calcitonin. The composition may be a solution, dispersion, powder or microspheres. Other enhancers, such as lysophosphatidylcholine, can be included if desired.

Abstract: Particles of a drug are directed away from the reticuloendothelial system by the use of surface coating and surface grafting techniques which substantially prevent the take up of the composite particles by the liver.