Cisplatin-loaded, Sialyl Lewis X-Modified Liposomes: Drug Release, Biodistribution and Antitumor Efficacy

Anticancer Res. 2017 Nov;37(11):6055-6061. doi: 10.21873/anticanres.12053.

Abstract

Background/aim: The aim of this study was to evaluate the characteristics of two cisplatin (CDDP)-loaded, sialyl Lewis X-modified liposomes (CDDP-SLX-LIP) with different particle size. Each had the same lipid composition and CDDP concentration, but a different drug-to-lipid ratio.

Materials and methods: The amount of platinum in the filtrates was determined by the ICP method. The antitumor effect was assessed using rats bearing MRMT-1 tumor.

Results: CDDP release was faster from the larger liposome formulation (L-LIP) than from the smaller one (S-LIP). Treatment with the two CDDP-SLX-LIPs resulted in comparable antitumor effects without obvious side-effects, but treatment with CDDP solution resulted in significant weight loss and an elevated BUN. Tumor accumulation of CDDP-SLX-LIP was clearly greater than that of CDDP solution and accumulation of S-LIP was greater than that of L-LIP.

Conclusion: CDDP-SLX-LIP exhibited antitumor effects depending on their release behavior and tumor accumulation.

Keywords: Cisplatin; accumulation; liposome; release; sialyl Lewis X.

MeSH terms

  • Animals
  • Antineoplastic Agents / administration & dosage*
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / pharmacokinetics
  • Apoptosis
  • Cell Proliferation
  • Cisplatin / administration & dosage*
  • Cisplatin / chemistry
  • Cisplatin / pharmacokinetics
  • Drug Liberation*
  • Female
  • Liposomes / administration & dosage*
  • Liposomes / chemistry
  • Mammary Neoplasms, Experimental / drug therapy*
  • Mammary Neoplasms, Experimental / pathology
  • Oligosaccharides / chemistry*
  • Rats
  • Rats, Sprague-Dawley
  • Sialyl Lewis X Antigen
  • Tissue Distribution

Substances

  • Antineoplastic Agents
  • Liposomes
  • Oligosaccharides
  • Sialyl Lewis X Antigen
  • Cisplatin