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Molecules 2012, 17(3), 3484-3500; doi:10.3390/molecules17033484

Synthesis and Preliminary Investigations of the siRNA Delivery Potential of Novel, Single-Chain Rigid Cationic Carotenoid Lipids

1
Pre-Medical Unit, Weill Cornell Medical College in Qatar, Doha, P.O. Box 24144, Qatar
2
Research Division, Weill Cornell Medical College in Qatar, Doha, P.O. Box 24144, Qatar
3
Department of Chemistry, Norwegian University of Science and Technology (NTNU), 7491 Trondheim, Norway
4
Department of Chemistry, Chemical Biology & Biomedical Engineering, Stevens Institute of Technology, Hoboken, NJ 07030, USA
These authors contributed equally to this work.
*
Author to whom correspondence should be addressed.
Received: 29 February 2012 / Revised: 12 March 2012 / Accepted: 12 March 2012 / Published: 16 March 2012
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Abstract

The success of nucleic acid delivery requires the development of safe and efficient delivery vectors that overcome cellular barriers for effective transport. Herein we describe the synthesis of a series of novel, single-chain rigid cationic carotenoid lipids and a study of their preliminary in vitro siRNA delivery effectiveness and cellular toxicity. The efficiency of siRNA delivery by the single-chain lipid series was compared with that of known cationic lipid vectors, 3β-[N-(N',N'-dimethylaminoethane)carbamoyl]-cholesterol (DC-Chol) and 1,2-dimyristoyl-sn-glyceryl-3-phosphoethanolamine (EPC) as positive controls. All cationic lipids (controls and single-chain lipids) were co-formulated into liposomes with the neutral co-lipid, 1,2-dioleolyl-sn-glycerol-3-phosphoethanolamine (DOPE). Cationic lipid-siRNA complexes of varying (+/−) molar charge ratios were formulated for delivery into HR5-CL11 cells. Of the five single-chain carotenoid lipids investigated, lipids 1, 2, 3 and 5 displayed significant knockdown efficiency with HR5-CL11 cells. In addition, lipid 1 exhibited the lowest levels of cytotoxicity with cell viability greater than 80% at all (+/−) molar charge ratios studied. This novel, single-chain rigid carotenoid-based cationic lipid represents a new class of transfection vector with excellent cell tolerance, accompanied with encouraging siRNA delivery efficiency.
Keywords: carotenoid lipids; single-chain; rigid; cationic; non-viral siRNA delivery carotenoid lipids; single-chain; rigid; cationic; non-viral siRNA delivery
This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).

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MDPI and ACS Style

Pungente, M.D.; Jubeli, E.; Øpstad, C.L.; Al-Kawaz, M.; Barakat, N.; Ibrahim, T.; Khalique, N.A.; Raju, L.; Jones, R.; Leopold, P.L.; Sliwka, H.-R.; Partali, V. Synthesis and Preliminary Investigations of the siRNA Delivery Potential of Novel, Single-Chain Rigid Cationic Carotenoid Lipids. Molecules 2012, 17, 3484-3500.

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