Lipid-complexed camptothecin: Formulation and initial biodistribution and antitumor activity studies Academic Article Article uri icon


MeSH Major

  • Adenocarcinoma
  • Antineoplastic Combined Chemotherapy Protocols
  • Breast Neoplasms


  • Water-soluble derivatives of camptothecin, and active topoisomerase I inhibitor, have shown a broad spectrum of activity against human tumors. Early clinical trials with the water-soluble sodium salt of camptothecin were hindered by significant cystitis, gastroenteritis, and leukopenia. Furthermore, the sodium salt of camptothecin has been shown to have significantly less activity than the water-insoluble lactone form of the compound. We describe a formulation of lipid-complexed CPT (LC-CPT; particle size range 20.8-208.1 nm) that is very easy to prepare and allows for intravenous administration in vivo in clinically relevant lipid-drug ratios (12.5:1 w/w). The lipid formulation had in vitro antitumor activity similar to that of CPT formulated without lipids and displayed similar cytotoxicity against MDR-1-negative and -positive tumor cells. The biodistribution of CPT was profoundly affected by lipid complexation; free CPT achieved the greatest concentration in the pulmonary parenchyma while LC-CPT achieved the highest concentration in the gastrointestinal tract. LC-CPT had significant antitumor activity in vivo against intraperitoneal L1210 and P338 leukemia and appeared to be more potent then free CPT.

publication date

  • March 14, 1996



  • Academic Article


Digital Object Identifier (DOI)

  • 10.1007/s002800050425

PubMed ID

  • 8612306

Additional Document Info

start page

  • 531

end page

  • 8


  • 37


  • 6