PMID: 8599866Jan 1, 1996Paper

In vivo antitumor activity of cis-bis-neodecanoato-trans-R,R-1, 2-diaminocyclohexane platinum(II) formulated in long-circulating liposomes

Cancer Chemotherapy and Pharmacology
A MoriL Huang

Abstract

A lipophilic cisplatin derivative, cis-bis-neodecanoato-trans- R,R-1,2-diaminocyclohexane platinum (II) (NDDP), was formulated in liposomes composed of phosphatidylcholine (PC) and cholesterol (Chol) additionally containing monosialoganglioside (Gm1) or polyethyleneglycol conjugated to phosphatidylethanolamine (PEG-PE). These NDDP-containing long-circulating liposomes were examined for in vivo antitumor activity using the mouse RIF-1 solid tumor as a target residing outside the reticuloendothelial system (RES). Biodistribution studies, using C3H/HeJ mice and 111In-labelled DTPA-SA as a lipid marker, showed that the activity of GM1 and PEG-PE in prolonging the circulation times of liposomes was preserved in the presence of 3.0 mol% of NDDP in the liposome membranes. The high levels of liposomes remaining in the blood for PC/Chol/GM1 and PC/Chol/PEG3000-PE liposomes were associated with high levels of platinum in the blood as determined by atomic absorption spectrophotometry. These NDDP-containing long-circulating liposomes showed approximately a three-fold increase in tumor accumulation as compared to the conventional PC/Chol liposomes. In vitro cytotoxicity studies using RIF-1 tumor cells showed that the presence of PEG-PE, but...Continue Reading

References

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Citations

Jun 6, 2000·Advanced Drug Delivery Reviews·P TardiT O Harasym
Jun 6, 2000·Advanced Drug Delivery Reviews·O V GerasimovD H Thompson
Sep 12, 2013·International Journal of Nanomedicine·Demin LiuWenbin Lin
Sep 1, 1996·Cancer Treatment Reviews·M RansonJ Margison
Jan 25, 2003·The Journal of Pharmacy and Pharmacology·Kevin J HarringtonRichard G Vile
Apr 22, 2018·European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Für Pharmazeutische Verfahrenstechnik E.V·Rea D SignorellJean-Christophe Leroux
Apr 5, 2000·Clinical Oncology : a Journal of the Royal College of Radiologists·K J HarringtonJ S Stewart
Mar 21, 2008·Journal of Pharmaceutical Sciences·Daryl C DrummondDmitri B Kirpotin

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