a composition comprising pharmacologically active agent particles, use thereof, intravenous catheter, sealed vial and emulsion comprising a pharmacologically active agent

摘要

a composition comprising pharmacologically active agent particles, use thereof, intravenous catheter, sealed vial and emulsion comprising a pharmacologically active agent. According to the present invention there are provided compositions and processes for in vivo release of substantially water-insoluble pharmacologically active agents (such as anticancer drug paclitaxel) in which the pharmacologically active agent is released in the form of protein coated suspended particles (which act as a stabilizing agent). In particular, the protein and pharmacologically active agent in a biocompatible dispersing medium are subjected to high shear in the absence of any conventional surfactant and also in the absence of any polymeric core material for the particles. The procedure produces particles smaller than 1 micron in diameter. The use of specific composition and preparation (eg addition of a polar solvent to the organic phase) and careful selection of the appropriate organic phase allows reproducible production of especially small nanoparticles less than 200 nm in diameter which can be filtered under sterile conditions. The particle system produced according to the present invention may be converted into a redispersible dry shovel comprising protein-coated water-insoluble drug nanoparticles and a free protein to which the molecules of said pharmacologically active agent are associated. This results in a unique delivery system in which part of the pharmacologically active agent is readily bioavailable (in the form of protein-bound molecules) and part of the agent is present within particles without any polymeric matrix.