Some aspects of liposomal oxaliplatin formulations

Abstract

Methods for creations of oxaliplatin liposomal form in laboratory scale are discussed in this mini-review. Analysis of existed methods has been carried out, and the estimation of their usage in pharmaceutical industry view has been given. Oxaliplatin is one of the modern anticancer medicines, which is used both in monotherapy and in combination with other anticancer agents. One of the disadvantages of oxaliplatin as an anticancer drug is high neuro- and cardiotoxicity, which can be reduced by the creation of its liposomal form. In most methods, PEG-conjugated lipids were used as a part of phospholipids’ bilayer. Cationic liposomes modified with DSPE (distearoyl phosphatidyl ethanolamine)-PEG2000, with composition PC (phosphatidyl choline)/ Chol (cholesterol)/DSPE-PEG2000 (2/1/0.2 molar ratio) showed in vivo higher efficiency against human carcinoma SW480 line on mice both in comparison with a control group and with a free oxaliplatin treated group. Moreover, the absence of cachexia, in case of liposomal oxaliplatin was noted. Also, the influence of Chol on liposomes stability was studied. It was discovered that addition of 40% mol of Chol to liposomes with HSPC (hydrogenated soybean PC)/DSPCPEG 2000 increased encapsulation by 8% within 24 h at 37°C. Comparison of trehalose and L-arginine for liposomes HSPC/Chol/PEG2000 was carried out. Both cryoprotectors showed appropriate stability results in a ratio of 1 : 4 to lipids. As a conclusion, liposomal oxaliplatin is a prospective medicine with less toxicity and higher efficiency against tumors in comparison with a free oxaliplatin.

Keywords

• oxaliplatin, phospholipids, drug substances, liposomal preparations, pharmaceutical industry