An organic solvent-free process for preparing a lipid formulation of an active compound, wherein said process comprises: a) preparing a suspension comprising at least one active compound and at least one lipid in a first aqueous medium at a pH between about pH 4.0 and pH 8.0, wherein said preparing of said suspension comprises a process consisting of: i) providing: 1) a first aqueous medium consisting of water or water having buffer dissolved in it, 2) at least one partially water-soluble or water-insoluble active compound, 3) at least one phospholipid and at least one lipid selected from the group consisting of cholesterol or cholesterol sulfate and salts thereof, cholesterol hemisuccinate and salts thereof, cholesterol phosphate and salts thereof; and 4) one or more cryoprotectants; ii) to said first aqueous medium, adding the at least one active compound and the at least one lipid; and iii) mixing said first aqueous medium, said at least one active compound, and said at least one lipid to form a suspension; b) treating said suspension to form a lipid-compound suspension, comprising lipid-compound complexes having a defined particle size; c) lyophilizing said lipid-compound suspension comprising lipid-compound complexes having defined particle size in the presence of one or more cryoprotectants to form lyophilized material; and d) reconstituting said lyophilized material with a second aqueous medium to obtain a lipid formulation of an active compound, said lipid formulation comprising a suspension of lipid-compound complexes of defined particle size, said defined particle size having a mean particle size of less than 5 microns. a) preparing a suspension comprising at least one active compound and at least one lipid in a first aqueous medium at a pH between about pH 4.0 and pH 8.0, wherein said preparing of said suspension comprises a process consisting of: i) providing: 1) a first aqueous medium consisting of water or water having buffer dissolved in it, 2) at least one partially water-soluble or water-insoluble active compound, 3) at least one phospholipid and at least one lipid selected from the group consisting of cholesterol or cholesterol sulfate and salts thereof, cholesterol hemisuccinate and salts thereof, cholesterol phosphate and salts thereof; and 4) one or more cryoprotectants; ii) to said first aqueous medium, adding the at least one active compound and the at least one lipid; and iii) mixing said first aqueous medium, said at least one active compound, and said at least one lipid to form a suspension; i) providing: 1) a first aqueous medium consisting of water or water having buffer dissolved in it, 2) at least one partially water-soluble or water-insoluble active compound, 3) at least one phospholipid and at least one lipid selected from the group consisting of cholesterol or cholesterol sulfate and salts thereof, cholesterol hemisuccinate and salts thereof, cholesterol phosphate and salts thereof; and 4) one or more cryoprotectants; 1) a first aqueous medium consisting of water or water having buffer dissolved in it, 2) at least one partially water-soluble or water-insoluble active compound, 3) at least one phospholipid and at least one lipid selected from the group consisting of cholesterol or cholesterol sulfate and salts thereof, cholesterol hemisuccinate and salts thereof, cholesterol phosphate and salts thereof; and 4) one or more cryoprotectants; ii) to said first aqueous medium, adding the at least one active compound and the at least one lipid; and iii) mixing said first aqueous medium, said at least one active compound, and said at least one lipid to form a suspension; b) treating said suspension to form a lipid-compound suspension, comprising lipid-compound complexes having a defined particle size; c) lyophilizing said lipid-compound suspension comprising lipid-compound complexes having defined particle size in the presence of one or more cryoprotectants to form lyophilized material; and d) reconstituting said lyophilized material with a second aqueous medium to obtain a lipid formulation of an active compound, said lipid formulation comprising a suspension of lipid-compound complexes of defined particle size, said defined particle size having a mean particle size of less than 5 microns.