Efficient nucleic acid transduction with lipoplexes containing novel piperazine- and polyamine-conjugated cholesterol derivatives

Heterocyclic amine-modified polyethylenimine as gene carriers for transfection of mammalian cells

“…Liposomes containing heterocyclic amines such as489 imidazole, pyridine and piperazine as the cationic head-groups 490 usually offered higher gene expression and lower cytotoxicity 491[42][43][44][45][46]. Nanoparticles prepared with PEI cross-linked with492 piperazine-containing linkers, piperazine-N,N 0 -dibutyric acid and 493 piperazine-N,N 0 -dipropanal, showed low toxicity and considerable 494 increase in transfection efficiency compared to PEI [47].…”

Inhibition of replication of hepatitis B virus in transgenic mice following administration of hepatotropic lipoplexes containing guanidinopropyl-modified siRNAs

“…Nevertheless, lipoplexes should have several important features before they may be considered efficient vehicles for hepatotropic delivery of anti-HBV siRNAs. Complexes need to be stable, enhance the half-life of siRNAs in the circulation, be positively charged and ensure targeted delivery to the liver [9,36,37]. The size and charge of lipoplexes are also critical for efficient hepatotropic delivery.…”

“…Stable nucleic acid lipid particles (SNALPs) delivered gene silencers efficiently in vivo to inhibit HBV replication in murine models of the viral infection [8]. Other lipoplex formulations have included polyamine-conjugated cholesterol [9] or aminoxycholesterol lipid to facilitate post coupling of 'stealth' polyethylene glycol moieties [10]. Recently, synthetic anti-HBV siRNAs have been delivered in vivo using Dynamic PolyConjugates (DPCs) [11,12].…”

Stimulation of Phospholipase D in HepG2 Cells After Transfection Using Cationic Liposomes

“…[7][8][9] Several derivatives of hydrophobic cholesterol (Chol) having cationic headgroups such as polyamine and guanidinium have been synthesized and tested for their utility. 10,11 We have also developed the cationic Chol derivatives that are linked to Llysinamide, L-ornithinamide and polyamidoamine by solidphase synthesis method.…”