Cationic niosomes an effective gene carrier composed of novel spermine-derivative cationic lipids: effect of central core structures

Abstract

Context: Cationic niosomes formulated from Span 20, cholesterol (Chol) and novel spermine-based cationic lipids of multiple central core structures (di(oxyethyl)amino, di(oxyethyl)amino carboxy, 3-amino-1,2-dioxypropyl and 2-amino-1,3-dioxypropyl) were successfully prepared for improving transfection efficiency in vitro. The niosomes composed of spermine cationic lipid with central core structure of di(oxyethyl)amino revealed the highest gene transfection efficiency.

Objectives: To investigate the factors affecting gene transfection and cell viability including differences in the central core structures of cationic lipids, the composition of vesicles, molar ratio of cationic lipids in formulations and the weight ratio of niosomes to DNA.

Methods: Cationic niosomes composed of nonionic surfactants (Span20), cholesterol and spermine-based cationic lipids of multiple central core structures were formulated. Gene transfection and cell viability were evaluated on a human cervical carcinoma cell line (HeLa cells) using pDNA encoding green fluorescent protein (pEGFP-C2). The morphology, size and charge were also characterized.

Results and discussion: High transfection efficiency was obtained from cationic niosomes composed of Span20:Chol:cationic lipid at the molar ratio of 2.5:2.5:0.5 mM. Cationic lipids with di(oxyethyl)amino as a central core structure exhibited highest transfection efficiency. In addition, there was also no serum effect on transfection efficiency.

Conclusions: These novel cationic niosomes may constitute a good alternative carrier for gene transfection.

• Cationic niosomes
• central core structures
• gene transfection
• spermine derivatives

Declaration of interest

The authors report no conflicts of interest. The authors alone are responsible for the content and writing of the paper. The authors wish to thank the Silpakorn University Research and Development Institute for financial support (Grant No. SURDI 58/01/03). NN acknowledges the Royal Golden Jubilee PhD program of TRF for studentship (Grant No. PHD/0217/2552). Higher Education Research Promotion (HERP) Program, Office of the Higher Education Commission and Center of Excellence for Innovation in Chemistry (PERCH-CIC) are gratefully acknowledged.