Application and safety analysis of DOTAP, a key excipient for nucleic acid delivery

DOTAP, one of the key excipients for nucleic acid delivery, has been widely loved as a phospholipid used in cationic liposomes. This issue of AVT xiaobian will start with DOTAP application and security for you to analyze DOTAP!

DOTAP is a amphiphilic molecule, mainly composed of three parts: polar head (hydrophilic group), connecting bond, hydrophobic tail.

The polar head of DOTAP, which is usually composed of tertiary amine or quaternary ammonium salt, is combined with negatively charged DNA molecules through electrostatic action. Later, imidazole head and amino acid head were studied. The polar head has an important effect on the loading efficiency and cytotoxicity of nucleic acid molecules. The greater the dosage of DOTAP in the prescription, the greater the drug loading, but the higher the zeta potential, the greater the cytotoxicity, the safety of the preparation is affected, the two need to balance. Colleagues in the academic department have studied toxicity in mice: immediate death by injection is possible when zeta potential is higher than +50mV. For the encapsulation of chemotherapeutic drugs, drug loading does not depend on DOTAP. Other neutral phospholipids such as DSPC and DPPC can be added to the prescription, which is less limited in dose.

The first commercial use of DOTAP was as a transfection agent. The polar head of DOTAP combines stably with negatively charged DNA molecules through electrostatic action, and the two can spontaneously form a stable complex after mixing. This method of transfection is very mild, can avoid the cytotoxic effects of lipid transfection or other transfection methods, and the transfection efficiency is higher than other lipid reagents.

At present, the more successful application cases of DOTAP include endotag-1, a cationic liposome of paclitaxel, and Endotag-2, a cationic liposome of camptoximin. It is also widely used as the transfection agent of Youxiu. The effect of RNA drugs is closely related to the selection of cationic lipid materials. When encountering problems in the experiment, it is advisable to try several cationic lipid materials.

For more information on key excipatory materials for nucleic acid delivery, please pay attention to our official website avt-avt.com or call our 400 official telephone number: 400-6262-623. We look forward to your consultation!