Physicochemical/structural investigation of lipid nanoparticles with high lecithin amounts loaded with patent protected pyrazoloquinolinone ligand DK-I-60-3

Abstract

Lipid nanoparticles are being intensively investigated for the formulation of the drugs with poor solubility substances (1). They represent colloid dispersions of the particles with lipid matrix that is solid at room and body temperature. Because of the low capacity of triglycerides for the drug substances incorporation, alternatively, high amounts of lecithin could be added to increase the solubilization (2). This was used for the incorporation of DK-I-60-3 (7- methoxy-d3-2-(4-methoxyd3-phenyl)-2,5-dihydro- 3Hpyrazolo[4,3-c]quinolin-3-one), novel deuterated pyrazoloquinolinone ligand, with very low solubility in water as well as in oils (3,4). However, because of amphiphilic nature of lecithin, its localization within nanoparticles should be analyzed, especially with respect to stability, drug loading capacity and drug localization, because it may additionally influence the drug release mechanism (2).