Lysosomal Trapping (Lysosomotropism)

• Lysosomes are essential for the degradation of old organelles and engulfed microbes and also play a role in programmed cell death¹.
• Lysosomotropic agents e.g., chloroquine, accumulate preferentially in the lysosomes of cells in the body.
• These agents tend to have both lipophilic or amphiphilic compounds with basic moieties. Once inside the acidic environment of the lysosome, the drug becomes protonated and trapped in the organelle².
• Trapping of drugs in the lysosome may be one mechanism leading to drug-induced phospholipidosis for cationic amphiphilic drugs (CAD).
• Cyprotex’s lysosomal trapping service is a cell based assay which uses high content screening to identify both lysosomotropism and cytotoxicity according to a recently published method².

Known lysosomotropic and non-lysosomotropic agents were screened in the lysosomal trapping assay. Data generated were compared to those published in the literature.

_{1) Turk B and Turk V (2009) J Biol Chem 284; 21783-21787
2) Nadanaciva S et al., (2011) Toxicology In Vitro 25; 715-723
3) Kazmi F et al., (2013) Drug Metab Dispos 41; 897-905}