Formulation of Cationic Niosomes for Gene Delivery: Effect of Molar Ratio of Cationic Lipid and Weight Ratio of Niosome/DNA Complexes

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Lalita Leksantikul
Nattisa Niyomtham
Theerasak Rojanarata
Tanasait Ngawhirunpat
Boon-ek Yingyongnarongkul
Praneet Opanasopit

Abstract

Introduction:  Niosomes, non-ionic surfactant vesicles, have been widely used in pharmaceutical field as a drug and biological delivery system. The cationic lipids can generate positive charge on the surface of niosomes that make niosomes suitable for gene delivery. However, usage cationic lipid in high concentration may cause of toxicity and low transfection efficiency. The aim of this study was to investigate the effect of the molar ratio of spermine derivative-cationic lipid (Ay) in the cationic niosome formulations and the weight ratio of cationic niosomes/DNA complex on the transfection efficiency and the cytotoxicity in human cervical carcinoma cells (HeLa cells) using pDNA encoding green fluorescent protein (pEGFP-C2). Materials and Method: Various formulations of cationic niosomes were prepared from Tween 61, cholesterol and cationic lipid (Ay) at the molar ratio of 2.5:2.5:1, 2.5:2.5:1.5 and 2.5:2.5:2 using thin film hydration with sonication method. The measurements of size and zeta potential as well as gel retardation assay were performed in order to characterize the suitable weight ratio of cationic niosome/DNA complexes. Results: the transfection efficiency of these cationic niosomes was in the following order: niosomes (2.5:2.5:1) > niosomes (2.5:2.5:1.5) > niosomes (2.5:2.5:2). The highest transfection efficiency was observed in the formulation of niosomes at the molar ratio of (2.5:2.5:1) and the weight ratio of 10, moreover this formulation was safe in vitroConclusion: The molar ratios of cationic lipid in the cationic niosome formulations and weight ratios of cationic niosomes/DNA complexes are the important factor for transfection efficiency and cytotoxicity.

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Pharmaceutical Sciences

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