Introduction to the Applications of DOPC and Cholesterol

DOPC and cholesterol application case study 1: Liposome LE-SN38

SN-38-Liposome LE-SN38 is a well-known drug, and I believe everyone is familiar with the characteristics of camptothecin drugs. Because of its stability and other reasons, the application of the active metabolite SN-38 has been restricted for a long time, but after the development of LE-SN38 liposome, many problems can be easily solved.

The project was developed by the emerging liposome technology company Neopharm, whose core technology is the use of artificially synthesized phospholipids - Four Nitrocellulose Glyceryl Phospholipids in the preparation of liposomes. Due to the unique properties of phospholipids, it can strongly interact with SN-38, stabilizing the drug by embedding it in the lipid membrane of the liposome, and thereby improving the stability of the drug and the formulation in vivo and in vitro. In addition to phospholipids, the prescription also includes DOPC and cholesterol. The drug-lipid ratio is about 1:18, with a particle size of 150-200nm, and an encapsulation rate of up to 95%.

Neopharm has developed four products based on this patented technology: LE-SN38, LE-rafAON (antisense nucleic acid), LEM (mitoxantrone), and LEP (paclitaxel). Among them, LE-SN38 is currently undergoing a phase II clinical trial in the United States for the indication of metastatic colorectal cancer.

DOPC and cholesterol application case study 2: Paclitaxel liposome LEP-ETU

I have introduced paclitaxel liposome EndoTAG-1 to you before. This time, I will tell you about paclitaxel liposome LEP-ETU. LEP-ETU is the paclitaxel liposome developed by NEOPHARM based on cardiolipin prescription. The sealing rate can reach more than 85%. ETU stands for "easy-to-use", because the product does not require pre-injection of desensitizers and there are not many restrictions on infusion speed. In addition to cardiolipin, DOPC and cholesterol are also used in the prescription. The clinical indication is ovarian cancer and the FDA has approved its orphan drug qualification.

As the unique weapon of the nano drug delivery system, cardiolipin can strongly interact with lipophilic drugs and stably embed the drug in the liposome phospholipid membrane, thereby improving the drug loading efficiency and the stability of the preparation in vivo and in vitro. Therefore, for the development of liposome formulations of poorly water-soluble drugs, such as paclitaxel, cardiolipin has played a crucial role.

In addition to LE-SN38 and LEP-ETU, Neopharm has also developed LE-rafAON (antisense nucleic acid) and LEM (mitoxantrone) based on cardiolipin patented technology, both of which have achieved good initial research results.

The disclosed clinical trial results show that LEP-ETU subjects are well tolerated, including 1 patient with complete remission, 15 patients with partial remission, and 10 patients with stable disease (a total of 35 subjects with metastatic breast cancer). The administration regimen is: dose 275mg/m2, administration cycle three weeks.

AVT (Shanghai) Pharmaceutical Tech Co., Ltd has been focusing on the fields of injections such as liposomes, fat emulsions, micro-nano targeted agents, and biological agents for more than ten years. It has developed a unique sales model of "university + research institute + enterprise".