The most commonly used lipid of cationic liposomes is DOTAP and its safety

Cationic liposomes are one of the most studied vectors in gene therapy. Compared with viral vectors, cationic liposomes have multiple advantages as non-viral vectors. DOTAP is the most commonly used lipid in cationic liposomes research, so we need to pay attention to its safety! Follow the AVT xiaobian to understand!

DOTAP is the most commonly used cationic lipid in cationic liposome research. Common DOTAP (Cl), chemically named (1, 2-dioleoxypropyl) trimethyl ammonium chloride, molecular formula C42H80NO4Cl, molecular weight 698.6, a quaternary ammonium salt, is a positively charged amphiphilic lipid compound. Because the production process is different, some characters are light yellow waxy, and the DOTAP produced by the company with good technology is white powder, which is easier to weigh and other practical operations.

DOTAP is a cationic lipid material for medicinal injection. What is the basic information of DOTAP?

1. Chinese name: DOTAP

2, chemical name :(2, 3-two oleyl-propyl) - trimethylammonium chloride salt; (2, 3-dioleyl-propyl)- trimethyl ammonium chloride

3, molecular formula: C42H80NO4Cl

4. CAS Number: 132172-61-3

5. Grade: grade of medicinal reagent

6, use: cationic liposome

7. Structural formula:

Cationic liposomes most commonly used lipid DOTAP and its safety - Avito (Shanghai) Pharmaceutical Technology Co., LTD

8. Properties: white solid

9. Purity: 99%

10, molecular weight: 698.56

11, melting point: 35~38℃

12. Storage conditions: -20±5℃, shading and airtight

13, precautions: avoid contact with strong acid, strong base, strong oxidizing substances

Classification and application advantages of cationic liposomes

According to the different encapsulated API, cationic liposomes can be divided into two categories. One is the liposome containing nucleic acid drugs represented by mRNA and siRNA, which is the most widely studied and applied non-viral vector in gene therapy. The other is the liposome preparation containing small molecular anticancer drugs such as paclitaxel and camptothecin, which has the targeting of tumor new blood vessels and has a good effect on cancer under the action of dual mechanisms.

Cationic liposomes as non-viral vectors have the following advantages:

Protect the therapeutic gene from being degraded in the body circulation. The cationic liposomes can encapsulate DNA fragments, promote the fusion of complex with cell membrane, and increase the uptake and expression of DNA.

Gao Xiao crossed the cell membrane and nuclear membrane and transfected cells to express/silence genes.

If the indication is cancer, it can selectively adsorb on negatively charged new tumor vascular endothelial cells, and the anticancer effect is better.

Application of cationic lipid DOTAP

As mentioned above, DOTAP is a amphiphilic molecule, which is mainly composed of three parts: polar head (hydrophilic group), connecting bond, and hydrophobic tail. The polarity head of DOTAP, which is combined with negatively charged DNA molecules through electrostatic action, is usually composed of tertiary amine or quaternary ammonium salt. Later, imidazole head and amino acid head were studied. Its polar head has an important effect on the efficiency of nucleic acid molecule encapsulation and cytotoxicity. In the prescription, the higher DOTAP dosage, the higher drug loading, but the higher Zeta potential, the greater the cytotoxicity, the safety of the preparation is affected, the two need to balance. Colleagues in the academic department once conducted an experimental study on toxicity in mice: when zeta potential is higher than +50mV, immediate death by injection may occur. For encapsulated chemotherapeutic drugs, DOTAP is not dependent on drug delivery, and other neutral phospholipids such as DSPC and DPPC can be added in the prescription, which is less limited in dosage.

Earlier DOTAP applications in commercial products were transfection reagents. The polar head of DOTAP stably binds to negatively charged DNA molecules through electrostatic interaction, and the two spontaneously form stable complexes when mixed. This transfection method is mild, avoids the cytotoxic effects of lipid transfection or other transfection methods, and is more efficient than other lipid reagents.

At present, the successful application cases of DOTAP include paclitaxel cationic liposome Endotag-1 and cationic liposome Endotag-2 of camptothecin, which are also widely used as the transfection reagent of superior xiu. The effect of RNA drugs is closely related to the selection of cationic lipid materials. When you encounter problems in the experiment, you may as well try several cationic lipid materials.

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