DPPG2-based Thermosensitive Liposomes Encapsulating Doxorubicin DPPG2-TSL-DOX

**Semantic type:** Pharmacologic Substance

**Definition:** A temperature-sensitive liposomal formulation composed of phosphatidylglycerol-based thermosensitive liposomes (DPPG2-TSL) encapsulating the anthracycline antineoplastic antibiotic doxorubicin, with potential antineoplastic activity. Upon intravenous administration, the DPPG2-based thermosensitive liposomes encapsulating doxorubicin DPPG2-TSL-DOX circulate in the bloodstream, extravasate and are activated locally by applying regional hyperthermia (RHT), which increases the tumor temperature to between 41.5 and 44 degrees Celsius using an external heat source. The elevated temperature causes compositional changes in the liposomes, creating openings that allow for the release of encapsulated doxorubicin. Doxorubicin intercalates DNA, interferes with the activity of topoisomerase II, and causes DNA adducts and other DNA damage, resulting in tumor cell growth inhibition and apoptosis. This agent also interacts with cell membrane lipids causing lipid peroxidation. Compared to non-thermosensitive liposomes, lyso-thermosensitive liposomes deliver higher concentrations of a cytotoxic agent to a heat-treated tumor site while sparing normal tissues unexposed to heat treatment.

**Synonyms:** - DPPG2-TSL-DOX - DPPG2-based TSL-encapsulating Doxorubicin DPPG2-TSL-DOX