Phospholipid for Charge-reversible Lipid Nanoparticles to Deliver siRNA

RNA interference induced intracellularly by small interfering RNAs (siRNAs) consisting of 21 to 23 nucleobase pairs is considered a promising candidate for cancer therapy, as it inhibits gene expression by promoting the degradation of target messenger RNAs (mRNAs).¹⁾ DOP-DEDA is a charge-reversible phospholipid suitable for preparing lipid nanoparticles (liposomes) for siRNA delivery into cells. While conventional lipid nanoparticles for siRNA delivery are aggregated under physiological conditions because of loss of ionization, or require PEGylation, it has been reported that siRNA-encapsulated lipid nanoparticles composed of DOP-DEDA are always ionized and thus can be taken up into cancer cells.^2,3)

Related Product

D6219

DOP-DEDA

References

• 1) Evidence of RNAi in humans from systemically administered siRNA via targeted nanoparticles
  • M. E. Davis, J. E. Zuckerman, C. H. J. Choi, D. Seligson, A. Tolcher, C. A. Alabi, Y. Yen, J. D. Heidel, A. Ribas, Nature 2010, 464, 1067.
• 2) Charge-reversible lipid derivative: A novel type of pH-responsive lipid for nanoparticle-mediated siRNA delivery
  • Y. Hirai, R. Saeki, F. Song, H. Koide, N. Fukata, K. Tomita, N. Maeda, N. Oku, T. Asai, Int. J. Pharm. 2020, 585, 119479.
• 3) LIPID DERIVEATIVE FOR NUCLEIC ACID INTRODUCTION
  • T. Asai, N. Oku, N. Maeda, N. Fukata, K. Tomita, PCT Int. Appl. WO 2018190017, 2018.

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