Abstract

Pharmacodynamic experiments using KM (immune-competent) mice as tumor inoculation models found that pixantrone (Pix) solution has severe thymus toxicity. Moreover, Pix has no therapeutic effect on tumors, instead causing uncontrolled tumor growth and accelerating animal death. Therefore, this study developed a PEGylated Pix liposome (Pix-PL) and investigated relevant parameters: particle size, morphology, encapsulation efficiency (EE%), stability, in vitro release, cytotoxicity, pharmacokinetic kinetic behavior, and antitumor efficacy and toxicity in vivo. We found that Pix-PL has strong anti-tumor effect and effectively reduces the thymus toxicity of Pix. In conclusion, the novel liposomes have clinical development value.

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