Clinical development of liposome-based drugs: formulation, characterization, and therapeutic efficacy

Abstract

Research on liposome formulations has progressed from that on conventional vesicles to new generation liposomes, such as cationic liposomes, temperature sensitive liposomes, and virosomes, by modulating the formulation techniques and lipid composition. Many research papers focus on the correlation of blood circulation time and drug accumulation in target tissues with physicochemical properties of liposomal formulations, including particle size, membrane lamellarity, surface charge, permeability, encapsulation volume, shelf time, and release rate. This review is mainly to compare the therapeutic effect of current clinically approved liposome-based drugs with free drugs, and to also determine the clinical effect via liposomal variations in lipid composition. Furthermore, the major preclinical and clinical data related to the principal liposomal formulations are also summarized.

Keywords: PEGlated liposomes; cationic liposomes; temperature sensitive liposomes; therapeutic efficiency; virosomes.

Figure 1

Chemical structures of lipids in liposome formulations. Abbreviations: DOTAP, 1,2-dioleoyl-3-trimethylammonium propane; DPPC, dipalmitoylphosphatidylcholine; DOPA, 1,2-Dioleoyl-sn-Glycero-3-Phosphate; MSPC, monostearoylphosphatidylcholine; DPPG, dipalmitoylphosphatidylglycerol; DSPC, distearoylphosphatidylcholine; HSPC, hydrogenated soy PC; DMPG, l-α-dimyristoylphosphatidylglycerol; DMPC, 1-α-dimyristoylphosphatidylcholine; DOPC, 1,2-Dioleoyl-sn-glycero-3-phosphocholine; DOPE, dioleoyl phosphatidylethanolamine; DSPG, distearoylphosphatidylglycerol; PEG2000-DSPE, polyethylene glycol 2000-distearoylphosphatidylethanolamine.