Cisplatin-loaded, sialyl lewis x-modified liposomes: Drug release, biodistribution and antitumor efficacy

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.