Application of dipalmitoylphosphatidylglycerol DPPG-Na phospholipids in multivesicular liposomes

Dipalmitoylphosphatidylglycerol DPPG-Na, a synthetic phospholipid, do you know this pharmaceutical injection-grade excipient? When it comes to the application of DPPG-Na, the more common products are multivesicular liposomes, such as cytarabine multivesicular liposomes, morphine sulfate multivesicular liposomes, and bupivacaine multivesicular liposomes. What is the specific situation?

The preparation of multivesicular liposomes is inseparable from the interaction of phospholipids such as DPPG-Na in the prescription and DepofoamTM technology. This technology was proposed by Pacira Pharmaceuticals, Inc of the United States and applied to many products such as DepoDur®, Exparel®, and DepoMLX under development. DepofoamTM is a micron-level honeycomb phospholipid bilayer structure. When liposomes are prepared by the secondary emulsification method, if the oil phase contains triglycerides, Depofoam will be obtained, which can be used to deliver chemical drugs, proteins, DNA, etc. , The drug release time can be up to 30 days.

Some friends may not be familiar with DPPG-Na, a phospholipid. Let me first talk about the basic information of DPPG-Na, a medicinal phospholipid.

Product name: Dipalmitoylphosphatidylglycerol (for injection)

Chemical name: 1,2-Dipalmitoyl-sn-glycerol-3-[phosphate-rac-(1-glycerol), sodium salt]

English name: DPPG-Na

CAS Number: 67232-81-9

Registration Number: F20180000838

Molecular weight: 745

Molecular formula: C38H74O10PNa

Grade: medicinal injection grade

Applicable fields: liposome membrane material, emulsifier

Product performance: white powder. Soluble in chloroform/methanol=2/1 (v/v)

Storage conditions: below -20℃, shading and airtight

Synthetic phospholipid DPPG-Na, it is obvious that this is a PG synthetic phospholipid with a purity of up to 99%. The DPPG-Na product provided by AVT is a medicinal injection grade and is often used as a liposome membrane material and emulsifier. Having been deeply involved in the pharmaceutical excipients industry for more than ten years, the DPPG phospholipids supplied byAVT are qualified. The products have been registered in the CDE with registration number F20180000838. At the same time, our products have also been registered in the FDA with DMF number 32797. Phospholipids products have very high temperature requirements, and DPPG phospholipids also need to be stored in a dark and airtight environment below -20°C.

At the beginning of the article, the editor told you that the application examples of DPPG include glycocytidine multivesicular liposomes, morphine sulfate multivesicular liposomes, bupivacaine multivesicular liposomes, etc. Let's take a look at these in detail. Multivesicular liposomes:

1. Depocyt®

Cytarabine liposomes developed by SkyPharm Inc. were listed in the United States in 1999 and are mainly used for the treatment of neoplastic meningitis. After encapsulating cytarabine into liposomes, the number of administrations was reduced from once every two days to one every two weeks, which greatly improved the patient's compliance. Its prescription phospholipid composition is DOPC, DPPG, cholesterol and triolein. The product is a 5mL normal saline suspension, each containing 50mg cytarabine, 22mg cholesterol, 28.5mg DOPC, 5mg DPPG and 22mg cholesterol.

2.DepoDur®

The morphine sulfate liposome developed by SkyPharm Inc. was approved by the FDA in 2004 for preoperative anesthesia or labor analgesia. Its prescription phospholipid composition is DOPC, DPPG, cholesterol, tricaprylin and triolein. Each product contains 10mg/mL morphine sulfate, 4.2mg/mL DOPC, 0.9mg/mL DPPG, 0.3mg/mL tricaprylin and 3.3mg/mL cholesterol and 0.1mg/mL triolein.

3.Exparel®

Bupivacaine liposomes developed by Pacira Pharmaceuticals, Inc., approved by the FDA in 2011, are used for postoperative anesthesia and analgesia at surgical sites, and can prolong the drug release to 72 hours. A new PC-like phospholipid excipient DEPC was used in the prescription, which is unique among the marketed products based on DepoFoamTM technology. Its prescription phospholipid composition is DEPC, DPPG, cholesterol and tricaprylin. Each bottle contains bupivacaine 13.3mg/mL, DEPC 8.2mg/mL, DPPG 0.9mg/mL, cholesterol 4.7mg/mL, and tricaprylin 2.0mg/mL. In recent years, the market and sales of Exparel® have grown rapidly. In 2015, the total sales reached 240 million US dollars and are still rising.

The DPPG-Na phospholipids used in multivesicular liposomes series products are first introduced here. If you want to know more information about our products, welcome to call us at 400-6262 623!