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Nonionic Surfactant Vesicles Composed of Novel Spermine-Derivative Cationic Lipids as an Effective Gene Carrier In Vitro

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Abstract

In the present study, nonionic surfactant vesicles (niosomes) formulated with Span 20, cholesterol, and novel synthesized spermine-based cationic lipids with four hydrocarbon tails in a molar ratio of 2.5:2.5:1 were investigated as a gene carrier. The effects of the structure of the cationic lipids, such as differences in the acyl chain length (C14, C16, and C18) of the hydrophobic tails, as well as the weight ratio of niosomes to DNA on transfection efficiency and cell viability were evaluated in a human cervical carcinoma cell line (HeLa cells) using pDNA encoding green fluorescent protein (pEGFP-C2). The niosomes were characterized both in terms of morphology and of size and charge measurement. The formation of complexes between niosomes and DNA was verified with a gel retardation assay. The transfection efficiency of these cationic niosomes was in the following order: spermine-C18 > spermine-C16 > spermine-C14. The highest transfection efficiency was obtained for transfection with spermine-C18 niosomes at a weight ratio of 10. Additionally, no serum effect on transfection efficiency was observed. The results from a cytotoxicity and hemolytic study showed that the cationic niosomes were safe in vitro. In addition, the cationic niosomes showed good physical stability for at least 1 month at 4°C. Therefore, the cationic niosomes offer an excellent prospect as an alternative gene carrier.

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ACKNOWLEDGMENTS

The authors would like to acknowledge the Commission of Higher Education (Thailand), the Thailand Research Funds through the Golden Jubilee Ph.D. Program (grant nos. PHD/0092/2551 and PHD/0217/2552), the Office of the Higher Education Commission, Ministry of Education, the Thailand Research Fund (RMU5480003), and the Silpakorn University Research and Development Institute (SURDI 57/01/24) for financial support.

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Authors and Affiliations

  1. Pharmaceutical Development of Green Innovations Group (PDGIG), Faculty of Pharmacy, Silpakorn University, Nakhon Pathom, 73000, Thailand

    Orapan Paecharoenchai, Lalita Leksantikul, Tanasait Ngawhirunpat, Theerasak Rojanarata & Praneet Opanasopit

  2. Department of Chemistry and Center of Excellence for Innovation in Chemistry, Faculty of Science, Ramkhamhaeng University, Bangkok, 10240, Thailand

    Nattisa Niyomtham & Boon-ek Yingyongnarongkul

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  1. Orapan Paecharoenchai
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  2. Nattisa Niyomtham
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  3. Lalita Leksantikul
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  4. Tanasait Ngawhirunpat
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Correspondence to Boon-ek Yingyongnarongkul or Praneet Opanasopit.

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Paecharoenchai, O., Niyomtham, N., Leksantikul, L. et al. Nonionic Surfactant Vesicles Composed of Novel Spermine-Derivative Cationic Lipids as an Effective Gene Carrier In Vitro . AAPS PharmSciTech 15, 722–730 (2014). https://doi.org/10.1208/s12249-014-0095-x

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  • DOI: https://doi.org/10.1208/s12249-014-0095-x

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