Internal radiotherapy and dosimetric study for 111In/177Lu-pegylated liposomes conjugates in tumor-bearing mice

Remote Loading of 64Cu2+ into Liposomes without the Use of Ion Transport Enhancers

“…The estimated blood circulation half-life of 9.7 h in mice is in agreement with earlier reports, 11,12,23 and that no leakage of 64 Cu-DOTA from liposomes is observed in mice plasma ( Figure S1). Together, these results substantiate the in vivo stability of liposomes loaded with 64 Cu using the UAL method.…”

“…The new UAL method has major advantages compared to previous reported IAL methods, 4,[7][8][9][10][11][12] because of its simplicity, excluding the use of any ionophore. furthermore showed a dramatic increase in oil/water-partitioning of copper as pH was raised from 6.5 to 7.0.…”

“…[7][8][9][10][11][12] So far, only a few ionophore assisted loading (IAL) procedures have been developed for liposomal PET imaging applications. 1,12,13 Despite the generally high loading efficiencies, high radionuclide retention, rapid loading kinetics and successful in vivo liposomal performance there are disadvantages of using transporter molecules such as ionophores or lipophilic chelators (hereafter referred to as ionophores as a common term) for remote loading of radionuclides into liposomes.…”

“…Common practice is therefore to use ionophores to increase the trans-membrane ion diffusion rate, and thereby improve the loading kinetics of charged ions such as radionuclides into liposomes. [7][8][9][10][11][12][13] Despite previous knowledge and findings within this field, the present work describes a novel loading method of the PET radionuclide 64 Cu 2+ into liposomes, excluding the use of ionophores (an unassisted loading). In this method, 64 Cu 2+ (or copper) is added to preformed liposomes entrapping a high affinity copper chelator (Figure 1, left).…”

In vivo evaluation of PEGylated 64Cu-liposomes with theranostic and radiotherapeutic potential using micro PET/CT

“…Furthermore, to achieve an effective treatment, a T/M ratio of at least 3-5 should be reached [33]. [34]. While the 177 Lu-liposomes in this study showed essentially no leakage when incubated in serum, a significantly lower retention of radionuclides (83%) was observed in previous study [34].…”