PEGylatedLiposomes for Loading Hydrophobic Drugs (100nm,5.0 mL)

This pre-formed liposome product is created for post loading of hydrophobic small molecule compounds into liposomes. The process of drug incorporation is very straight-forward. Then simply add an aliquot of drug solution (prepared in a water-miscible solvent such as ethanol, DMSO and etc.) into the liposome suspension. The drug molecules can be incorporated into the lipid bilayers by the nature of hydrophobic interactions. The drug solubility therefore could be significantly enhanced. Liposomal drug concentration of 1-2 mg/mL could be achieved for most lipophilic drugs. PEGylation of the liposomes provides not only better formulation stability but also the potential of achieving prolongedin vivoblood circulation. The finished drug loaded formulations are suitable for either in vitro testing or in vivo studies.

Specifications

Lipids:Phosphatidylcholine and mPEG2000-DSPE (95:5 mol%)

Total lipid content.: 220 mgs in 5 mL

Lipid concentration: 50mM

Mean particle size:100 nm (90-120 nm)

Buffer solution:PBS pH7.0 – 7.4 (phosphate buffered saline)

Shelf-life: 6 months stored at 2-8 °C (guaranteed for non-drug loaded, replacement only)

Instructions

Method of Drug Loading

1. Prepare a concentrated drug solution (20-50x of the final targeted drug concentration) in a water-miscible solvent, such as ethanol, DMSO and etc.2.Aliquot out appropriate amount of the above reconstituted liposomes into a container suchas a 15 mL centrifuge tube3. Pre-warm the liposomes to 45-50°C in a water bath4.To the liposome solution, slowly add appropriate amount of the above drug solution(preferably using a positive displacement pipette for good accuracy) to the liposome solution while vortexing at medium speed5. Incubate drug/liposome mixture in the water bath with frequent mixing for 60 min6. The drug loading is completed.

Additional Information

1. Keep the final solvent content below 5%, since too much solvent may affect the integrity of the liposomes2. The solvent in the final formulation could be removed by dialysis or gel filtration column if necessary3. The final formulation could be sterile filtered for long term storage4. Some drugs post loading may gradually crystalize out over time, so it is advised to monitor the stability of the drug-loaded formulations5. The drug crystals can be monitored under optical microscope, though a more reliable analytical assay, i.e. HPLC, is desired6. The turbidity may increase slightly due to the incorporation of the drug. But if it becomes significantly cloudy, it may indicate the drug is over loaded.Reduce the drug/lipid ratio if this happens.

Drug Loading Optimization

1. The capacity of the liposomes for the hydrophobic drug loading really depends on the nature of the drug, so optimization is necessary to determine the maximum drug loading capacity.2. Conduct drug loading in small volumes at a series of increasing drug/lipid ratios3. The pH may also affect the drug loading, use a pH at where the drug is the most lipophilic, but keep in the range of 4-84. Observe the presence of drug crystals under microscopy and/or by centrifugation to pellet down the drug crystals5. Identify the maximum drug/lipid ratio at which no or minimal drug crystals seen6. It is recommended to monitor the stability for a period of time, because drug may crystalize out over time7. Conduct the final drug loading at or below the maximum drug/lipid ratio determined.

FormuMax供应主要产品： Clophosome -氯膦酸盐脂质体 FormuMax提供两种预埋有氯磷酸盐分子的中性脂质体产品，该产品单次静脉或腹腔注射后可在脾脏经巨噬细胞清除率可达80-90%，并具有高度活性、稳定的理化性质（长期冰箱存放后仍保持均一性及悬浮特性），粘滞度低使用简便，适用于静脉、腹腔、皮下、鼻腔、气管等多种方式给药。 Doxoves-盐酸多柔比星脂质体 FormuMax可提供脂质定制的盐酸多柔比星脂质体（定制内容为脂质成分及脂质体大小）。FormuMax提供的产品为Doxoves，具有高度的产品稳定性和一致性, 紧密的粒径分布和高效的药物包埋效率（高达4.0 mg/mL(40mM lipid)的包埋药物浓度）。 Doxoves系列产品在产品特性、稳定性及药代动力学特性上可媲美商业产品Doxil 。 Drug Loaded liposomes FormuMax提供多款包埋活性药物的脂质体产品，包括Doxorubicin HCl（含2.0mg/mL及4.0mg/mL两种浓度），Irinotecan HCl (2.0mg/mL)，Topotecan HCl (2.0mg/mL)，产品线仍在持续更新中。 预制脂质体 FormuMax 供应的预制脂质体产品囊括多种通用的脂质体类型，使用世界*的优质脂类原料。该系列产品易于使用，稳定性、可靠性及可重复性高，节省时间和成本，并可为研究人员提供定制脂质体服务。目前FormuMax提供聚乙二醇化/非聚乙二醇化的常用脂质体，以及含浓度梯度Ammonium的脂质体 阳离子脂质体 FormuMax供应一系列的阳离子脂质体，用于需带正电荷的脂质体或细胞转染质粒DNA、反义/干扰RNA等。 荧光脂质体 FormuMax 供应预制荧光标记的脂质体，包括常规荧光脂质体、生物素化的荧光脂质体以及Avdinized化的荧光脂质体，另外还提供客户定制的荧光脂质体（脂类及染料可选）。 脂质体制备薄膜 FormuMax 供应一系列不同规格的聚碳酸酯薄膜，用于脂质体挤出制备。