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Dicationic Amino Substituted Gemini Surfactants and their Nanoplexes: Improved Synthesis and Characterization of Transfection Efficiency and Corneal Penetration In Vitro.
Pharmaceutical Research ( IF 3.5 ) Pub Date : 2020-07-14 , DOI: 10.1007/s11095-020-02836-6 Lokesh Narsineni 1 , Marianna Foldvari 1, 2
中文翻译:
用阳离子阳离子氨基取代的双子表面活性剂及其纳米复合物:体外转染效率和角膜穿透性的改进合成与表征。
更新日期:2020-07-14
Pharmaceutical Research ( IF 3.5 ) Pub Date : 2020-07-14 , DOI: 10.1007/s11095-020-02836-6 Lokesh Narsineni 1 , Marianna Foldvari 1, 2
Affiliation
Purpose
To formulate and characterize nanoparticles from m-7NH-m gemini surfactants, synthesized by a new improved method, for non-invasive gene delivery including optimization of composition for transfection efficiency and corneal penetration.Methods
A one-pot, solvent-free, DMAP-free method was developed for the synthesis of m-7NH-m (m = 12–18) gemini surfactant series. Lipoplexes (LPXs) and nanoplexes (NPXs) of gemini surfactant-plasmid DNA were formulated with and without DOPE helper lipid, respectively, at various charge ratios and characterized by dynamic light scattering and zeta potential measurements. Transfection efficiency, cellular toxicity, effect of DOPE and gene expression kinetic studies were carried out in A7 astrocytes by flow cytometry and confocal microscopy. Corneal penetration studies of 18-7NH-18 NPXs were carried out using 3D EpiCorneal® tissue model.Results
The new synthesis method provides a two-fold improved yield and the production of a pure species of m-7NH-m without DMAP and trimeric m-7N(m)-m surfactants as impurities. Structure and purity was confirmed by ESI-MS, 1H NMR spectroscopy and surface tension measurements. Particle size of 199.80 ± 1.83 nm ± S.D. and a zeta potential value of +30.18 ± 1.17 mV ± S.D. was obtained for 18-7NH-18 5:1 ratio NPXs showed optimum transfection efficiency (10.97 ± 0.11%) and low toxicity (92.97 ± 0.57% viability) at the 48-h peak expression. Inclusion of DOPE at 1: 0.5 and 1:1 ratios to gemini surfactant reduced transfection efficiency and increased toxicity. Treatment of EpiCorneal® tissue model showed deep penetration of up to 100 μm with 18-7NH-18 NPXs.Conclusion
Overall, 18-7NH-18 NPXs are potential gene delivery systems for ophthalmic gene delivery and for further in vivo studies.中文翻译:
用阳离子阳离子氨基取代的双子表面活性剂及其纳米复合物:体外转染效率和角膜穿透性的改进合成与表征。