Delivery of the Radionuclide 131I Using Cationic Fusogenic Liposomes as Nanocarriers

Abstract

Liposomes are highly biocompatible and versatile drug carriers with an increasing number of applications in the field of nuclear medicine and diagnostics. So far, only negatively charged liposomes with intercalated radiometals, e.g., 64Cu, 99mTc, have been reported. However, the process of cellular uptake of liposomes by endocytosis is rather slow. Cellular uptake can be accelerated by recently developed cationic liposomes, which exhibit extraordinarily high membrane fusion ability. The aim of the present study was the development of the formulation and the characterization of such cationic fusogenic liposomes with intercalated radioactive [131I]I− for potential use in therapeutic applications. The epithelial human breast cancer cell line MDA-MB-231 was used as a model for invasive cancer cells and cellular uptake of [131I]I− was monitored in vitro. Delivery efficiencies of cationic and neutral liposomes were compared with uptake of free iodide. The best cargo delivery efficiency (~10%) was achieved using cationic fusogenic liposomes due to their special delivery pathway of membrane fusion. Additionally, human blood cells were also incubated with cationic control liposomes and free [131I]I−. In these cases, iodide delivery efficiencies remained below 3%.

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“…Recently developed cationic liposomes have accelerated cellular internalization, resulting from a high membrane fusion ability. Cationic liposomes are composed of a classical lipid mixture of neutral lipid 1,2-dioleoyl-sn-glycerol-3-phosphoethanolamine (DOPE) and cationic lipid 1,2-dioleoyl-3-trimethylamine propane (DOTAP), which are used as carrier particles to achieve optimal cargo delivery through the attractive interactions between positively charged liposome surface and negatively charged cargo (such as protein, peptide, or RNA molecules) [ 137 ]. An animal experiment reported that the mRNA encoding a tumor-associated antigen encapsulated by a cationic liposome complex was released at the target site after its intranasal administration in mice, which induced an immune response and prevented tumor growth [ 138 ].…”

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“…Owing to its high biocompatibility and non-toxicity, liposomes have been used as nano-drug carriers in tumor treatment [55]. Liang et al labeled a therapeutic radioisotope 131 I onto albumin-encapsulated liposomes to improve vasculature permeability and promote the enrichment of drugs within tumor, so as to enhance the anti-tumor efficacy of radionuclides [56].…”

“…In recent research, Kolašinac et al intercalated radionuclide 131 I into cationic fusogenic liposomes to form the novel nanocomposites. Compared with free iodine uptake, the usage of nanocomposites achieves a 10% increase in drug delivery efficiency with its special membrane fusion ability [55].…”