Byung Cheol Shin
Medical and Pharmaceutical Chemisty, University of Science and Technology, 52 , Eoeun-dong, Yuseong, Daejeon, 305-333, Republic of Korea

Abstract:

Objectives: Liposomes have been studied as carriers of magnetic resonance (MR) contrast agents to obtain extended MR images in tumor site. In this study, dual functional liposomes for chemotherapeutics and diagnostics were developed by efficient loading method for coencapsulation of gadolinium (Gd)-doxorubicin (Dox).

Methods: Gd-Dox loaded liposomes were prepared by ion gradient method based on Dox-metal complexation. The optimum formulation for efficient loading of Dox and Gd was determined according to various concentrations of hydrating Gd solution. Size and zeta potential of liposomes were characterized by electrophotometer light scattering (ELS) and Gd content was determined by inductively coupled plasma optical emission spectrometer (ICP-OES). The chemotherapeutic and MR properties of liposomes were evaluated in vitro.

Results: The optimized liposome coencapsulated 4.1mM of Dox and 11.8mM of Gd. Liposomally encapsulated Gd exhibited higher cellular uptake than MRbester® widely used for clinical diagnosis. Additionally, Dox of the liposome was highly internalized compared to Doxil®.

Conclusions: Highly internalized Gd-Dox of liposome could provide improved contrast sensitivity for molecular imaging and enhance the cancer killing effects. Our study suggests possibility of the liposome for therapeutic and diagnostic carrier.

Keywords: liposome / Gadolinium / drug delivery/ magnetic resonance imaging