Abstract: The invention relates to a method for the preparation of a carrier loaded with lipophilic biologically active substance based on reconstituted LDL (Low Density Lipoprotein), wherein (1) LDL is lyophilized in the presence of a protective agent; (2) the lyophilized LDL is extracted with an organic solvent; (3) the biologically active substance solubilized in a solvent is incubated with extracted LDL; the solvent is evaporated and the reconstituted LDL solubilized in an aqueous buffer; the non-incorporated biologically active substance is separated from the LDL-complex, characterized in that in step (1) the protective agent is a monosaccharide, a disaccharide, a water-soluble polysaccharide, a sugar alcohol or a mixture of these and in step (3) optionally the extract obtained during the extraction of the lyophilized LDL is mixed with the lipophilic biologically active substance solubilized in an organic solvent and this mixture is then incubated with the LDL.