Synthesis of novel cationic lipids for preparation of liposomes to be used in gene therapy of glioma

Abstract

The synthesis of a series of cationic lipids for the preparation of liposomes to be used in gene therapy is described. The synthetic strategy is designed in few steps and affords good yields.

Synthesis, gene transfection efficiency, and serum compatibility of β-sitosterol-based cationic lipids with different headgroups

“…3b-[(N 5 ,N 10 ,N 14 -Tri(tert-butyloxycarbonyl-(N 1 -sperminyl)))-carbonyloxy]b-sitosterol (13) and incubated at 37 1C under 5% CO 2 for 48 h. For the L2K transfection, the procedure followed the manufacturer's instructions. L2K/DNA complex was set at the weight ratio of 2.5 : 1.…”

“…In addition to the use in LNP, cationic lipids can form liposomes when suspended in water under appropriate conditions. 14 The negatively charged DNA can interact with cationic liposomes through electrostatic interactions leading to lipoplexes. 15 The DNA binding affinity of cationic liposomes are important for high efficacy of transfection.…”

Functional liposomes in the cancer-targeted drug delivery

“…Any lipophilic or amphiphilic components, integrated into the membranes, influence the functional complexity and biological characteristics of the membrane and the outer surface of the membrane. 131–133 Cationic lipids are composed of a charged head-group, comprising of a hydrophobic moiety and a linker (spacer, backbone) where this linker acts as a connector between hydrophobic domain and cationic head. The type of the spacer chain with regard to chain length, saturation and symmetry has an impact on membrane fluidity and thereby the transfection efficiency of the cationic liposomal systems.…”

“…Some of the used cationic lipids used in cationic liposomes are N-(2-hydroxyethyl)-N,N-dimethyl-2,3-bis(tetradecyloxy)-1-propanaminium bromide (DMRIE) and 3β-[N-(dimethylaminoethane) carbamoyl]cholesterol (DC-Chol). 132,134,135 Nucleic acid-based bioactive materials have recently emerged as a new class of next generation therapeutics. However, their development has been restricted due to the relatively weak delivery into target cells.…”

Function/structure correlation in novel pH-dependent cationic liposomes for glioma cells transfection in vitro

“…Cationic liposomes are also used as non-viral delivery systems in the gene therapy of glioma [10][11][12]. In the context of this research strategy, pH-dependency and transfection efficiency in rat C6 glioma cells line of seven novel liposomes [13] were studied. The corresponding lipids (Fig.…”