Targeting Stealth liposomes in a murine model of human small cell lung cancer

• Author(s): Moreira, João N. ; Gaspar, Rogério ; Allen, Theresa M.
• Date: 2001
• Persistent ID: http://hdl.handle.net/10316/5794
• Origin: Estudo Geral - Universidade de Coimbra
• Subject(s): Pegylated liposome; Doxorubicin; Targeting; Antagonist G; Small cell lung cancer
• Document Type: Article
• Language: English

Description

Tumor accumulation and therapeutic activity of Stealth liposomes loaded with doxorubicin (DXR) were examined in Balb/c nude mice xenografts inoculated subcutaneously with the human small cell lung cancer (SCLC) cell line, H69. Mice were treated with non-targeted liposomes (SL) or liposomes targeted with antagonist G coupled to the liposome surface (SLG). SLG showed 30-44-fold higher binding to H69 cells harvested from H69 xenografts than SL. At 48 and 72 h post injection, tumor accumulation of [125I]tyraminylinulin-containing liposomes was shown to be dependent on liposome size but independent of the presence of the targeting ligand. Maximum tumor uptake of either SLG or SL ranged from 2 to 4% of injected dose/g of tissue. In therapeutic studies, mice received three weekly injections of 3 or 6 mg free DXR/kg or 3 or 10 mg liposomal DXR/kg at initial tumor volumes of either 7 or 33 mm3. The therapeutic efficacy of DXR-containing SL or SLG was significantly improved over free DXR, but SLG did not improve anti-tumor efficacy relative to SL. Stealth liposomes containing DXR have potential as a therapy against human SCLC tumors. http://www.sciencedirect.com/science/article/B6T1T-447NS7N-4/1/553ad69a12cb515c11896a098d0065f7