Gemini Surfactants: A New Family of Building Blocks for Non-Viral Gene Delivery Systems

Abstract

Gemini surfactants provide a significant opportunity in the development of new non-viral delivery systems designed for gene therapy applications. This review summarizes the wide range of gemini surfactant structures that have been employed for DNA transfection in vitro. A general observation is that those structures capable of inducing a wide variety of polymorphic structures (lamellar, hexagonal, or cubic phases) demonstrate higher transfection efficiencies. Those compounds whose structures result in pH-dependent changes in aggregate structure similarly show higher levels of transfection. In vivo transfection using gemini surfactants has been demonstrated in only three cases, and in a recent study the transfection was linked to a specific therapeutic response.

Development of Dioctadecyldimethylammonium Bromide/Monoolein Liposomes for Gene Delivery

“…This negative effect was balanced with the appearance of helpers (DOPE) [74] and natural lipid-derivatives such as cholesterol [100] or glycerol [101], although sometimes compromising transfection efficiency. Gemini-dimeric surfactants also presented promising potential but with significant toxicological consequences [102][103][104][105][106].…”

New Amphiphilic Amino Acid Derivatives for Efficient DNA Transfection <i>in Vitro</i>

“…Except for the least active amphiphile, AG2-C 16 , all compounds showed two peaks of activity at N/P ratio of 15 and 28, respectively. Normally, most compounds of this type have a rising activity curve with a single maximum [11] [28] [34]. Although the reasons are not clear yet, we can assume that the low activity observed for all compounds atan N/P ratio of 15 can be because lipoplexesare still not fully formed.…”

Characterization of the host–guest complex of a curcumin analog with β-cyclodextrin and β-cyclodextrin–gemini surfactant and evaluation of its anticancer activity

“…Based on the affinity of the CD cavity to accommodate the gemini tail(s) of the CDgemini surfactant, the gemini moiety will be unavailable to form supramolecular assembly in the traditional manner of the gemini surfactants. 44 Moreover, contrary to the case of studies with free gemini surfactants, the constant mole ratio of gemini surfactant to CD moiety in CDgemini surfactant compounds leads to the result that increasing the concentration of CDgemini surfactant does not enhance self-assembly to form micellar structures. This can explain the fact that specific conductivity versus concentration profiles of the CDgemini surfactant (results not shown) do not have a sharp break point, the critical micelle concentration, consistent with that of gemini surfactant, alone.…”