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Anti-cancer activity of 9-nitrocamptothecin liposome aerosol in mice.

We have found that 9-nitrocamptothecin (9-NC) administered in a liposome formulation by small-particle aerosol is remarkably effective in the treatment of cancer in mice in doses that are several-fold lower than is required by other routes of administration. This favorable response was noted when used against human cancer xenografts implanted subcutaneously (1) and against human osteosarcoma cells given intravenously to produce experimental pulmonary metastases, all in the nude mouse model. B-16 murine melanoma cells given intravenously to produce pulmonary metastases also responded to the treatment. Pharmacokinetic (2) and toxicology studies (unpublished) were performed in mice and dogs. These studies suggested that the methodology might have application in treatment of cancer in humans. A report of these studies follows.