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What is the application of sucrose pharmaceutical excipients as freeze-drying protectants for lipid?



Sucrose, especially high-purity pharmaceutical sucrose, a common liposomal freeze-drying protectant, and a frequent visitor in research trials, this AVT editorial Introducing you to the use of sucrose as a liposomal lyophilization protectant.AVT brings you low endotoxin injectable grade sucrose!

Liposomes as drug carriers have the advantage of improving drug efficacy, reducing adverse drug reactions and targeting effects, but liposomes, especially The poor stability of liposomes prepared with lipids containing unsaturated bonds such as EPCs in aqueous media is an important limitation. In order to overcome the physical and chemical instability of liposomal preparations in long-term storage, we often freeze-dry the liposomal products, giving the The drug is then reconstituted into a liposomal suspension in an appropriate medium prior to administration.

In general, the membrane structure of the liposomal phospholipid bilayer is sensitive to freezing and drying processes: liposomal dehydration causes a shift in the liquid crystal state of the phospholipids to a more liquid state. The transition from the gel state, dry liposome rehydration is also accompanied by a transition from the gel to the liquid crystal state, both of which cause liposome content Leakage, increased particle size and the transition from single to multiple chambers are problems. It is therefore important to select a suitable freeze-drying protectant to reduce or eliminate liposome damage caused by the freeze-drying process.

In the freeze-drying process of liposomes, sucrose is the most commonly used kind of protective agent. Compared with mannitol, glucose, etc., it has a higher Tg and better viscosity protection, and is more cost-effective than algae sugar. Many of the liposomal extra-aqueous phases use sucrose, so that it is often preferred in order not to otherwise affect the preparation itself. The general dosage is 5%~10%.

The choice of freeze-drying protective agent is an important factor affecting the quality of freeze-drying. The freeze-drying process will lead to the aggregation and fusion of liposomes, accompanied by the leakage of liposome contents, while sucrose can play a role in reducing the film fusion, protects liposomal particles from rupture and drug leakage during lyophilization, and in addition acts as an excipient - a great influence on the The shape, looseness, and collapse of the cake after lyophilization are affected. A large body of literature has shown that the liquid stability and the effect of re-dissolution of liposomal preparations using sucrose as a lyophilization protectant (mainly drug Encapsulation rate and particle size variation) are both good. For example, the commercially available cytarabine + ruxomycin complex liposomal Vyxeos uses sucrose as a lyophilization protectant.

For injectables, sucrose also acts as an osmotic regulator, so if you have lyophilization needs, you may want to try it.

What is the application of sucrose pharmaceutical excipients as freeze-drying protectants for liposomes?-AVT (Shanghai) Pharmaceutical Tech Co., Ltd.

If you are interested in AVT's high purity, low endotoxin sucrose products, please contact us at 400-6262 623.