Cationic Lipid

The ionizable cationic lipid DLin-MC3-DMA is an effective vector for siRNA delivery. DLin-MC3-DMA (MC3) was discovered by Thomas Madden and Michael Hope during their exploration of novel ionizable lipids. It was used as a key component in Onpattro, the first siRNA drug approved by the FDA in 2018 (Onpattro also marks the first-ever targeted RNA-based gene therapy administered via a non-viral vector).

The ionizable cationic amino lipid SM-102 is commonly used to encapsulate and deliver nucleic acid (e.g., mRNA or siRNA) drugs as well as other bioactive substances and plays an important role in the development of mRNA therapeutics and vaccines with lipid nanoparticles (LNPs) as delivery carriers. It has also been used in the mRNA-LNP COVID-19 vaccine mRNA-1273 (Moderna).

ALC-0315 is an ionizable amino lipid that can significantly enhance the efficiency of LNP-mediated mRNA delivery and ensure effective mRNA escape from endosomes within cells, thereby enhancing gene transfection. As an ionizable cationic lipid approved for clinical RNA therapeutics, it has been utilized in the development of mRNA vaccines for COVID-19. It serves as the cationic lipid component in the BNT162b vaccine against COVID-19.

DC-CHOL is an effective steroid-based transfection agent and lipid formulation reagent. It is primarily employed in the preparation of various carriers, including microbubbles for contrast ultrasound ...

DOTAP is an effective cationic lipid, originally utilized in commercial products as a gene transfection reagent. It is also applicable as a pharmaceutical excipient in liposomal formulations. Its notable application is EndoTAG-1, a cationic liposomal formulation of paclitaxel. DOTAP imparts a positive charge to EndoTAG-1, allowing it to selectively adhere to tumor endothelial cells (TECs) with negative charges. This selective adsorption facilitates targeted attack on tumor neovasculature without harming healthy vessels, effectively inhibiting tumor growth.

DOP-DEDA is a charge-reversible phospholipid suitable for preparing lipid nanoparticles (LNPs) for delivering siRNA into cells. Traditional LNPs used for siRNA delivery may aggregate under physiological conditions due to lack of ionization or PEGylation. It has been reported that siRNA-loaded LNPs formulated with DOP-DEDA are always ionized, thus enabling their uptake by cancer cells.

C12-200 is an ionizable cationic lipid and helper lipid. Its cationic properties enable it to effectively bind with negatively charged nucleic acids (such as mRNA), thus facilitating intracellular nucleic acid delivery. Research has proposed a method for preparing freeze-dried C12-200vmRNA LNPs utilizing a continuous freeze-drying technique based on spin-freezing.