Cationic nanoemulsions as potential carriers for intracellular delivery

• DOI: 10.1016/j.jsps.2014.07.007
• Publication Date: 2014-07-18T17:30:31Z
• Authors: P.V. Khachane; A.S. Jain; V.V. Dhawan; G.V. Joshi; A.A. Date; R. Mulherkar; M.S. Nagarsenker
• Keywords: Didodecyldimethylammonium bromide; Pharmacology; 0404 agricultural biotechnology; Nanoemulsion; Pharmaceutical Science; Original Article; Intracellular delivery; 04 agricultural and veterinary sciences; Cytosolic delivery; Cationic; 3. Good health

Successful cytosolic delivery enables opportunities for improved treatment of various genetic disorders, infectious diseases and cancer. Cationic nanoemulsions were designed using alternative excipients and evaluated for particle size, charge, effect of sterilization on its stability, DNA condensation potential and cellular uptake efficiency. Various concentrations of non-ionic and ionic stabilizers were evaluated to design formula for colloidally stable cationic nanoemulsion. The nanoemulsion comprised of 5% Capmul MCM, 0.5% didodecyldimethylammonium bromide (DDAB), 1% phospholipid, 1% Poloxamer 188 and 2.25% glycerol and possessed particle size of 81.6 ± 3.56 nm and 137.1 ± 1.57 nm before and after steam sterilization, respectively. DNA condensation studies were carried out at various nanoemulsion: DNA ratios ranging from 1:1 to 10:1. Cell uptake studies were conducted on human embryonic kidney (HEK) cell lines which are widely reported for transfection studies. The nanoemulsions showed excellent cellular uptake as evaluated by fluorescence microscopy and flow cytometry. Overall, a colloidally stable cationic nanoemulsion with good DNA condensation ability was successfully fabricated for efficient cytosolic delivery and potential for in vivo effectiveness.