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Liposome Lipid Ratio Screening

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We have been operating our Lipid Formulation Development Center for numerous years, demonstrating our extensive experience and expertise in this field. Our team of professional scientists offers specialized screening services to assist clients in determining the optimal lipid ratio. With our cutting-edge facilities, we have established a fully integrated pipeline that encompasses four service types: phospholipid type screening, phospholipid modification services, phospholipid addition ratio screening, and cholesterol ratio screening services.

The Importance of Liposome Lipid Ratio Screening

The properties of liposomes are primarily determined by the lipid characteristics, particularly the length and saturation of fatty acid chains in phospholipids. These factors can influence the phase transition temperature from gel to liquid crystal and the permeability of lipid bilayers to specific molecules. Unsaturated fatty acids have the potential to increase pore size and permeability, while saturated fatty acids enhance stability through tighter binding. Additionally, membrane quality is also influenced by fluidity, which varies based on the Tc value (phase transition temperature) of phospholipids and is affected by factors such as acyl chain length, hydrocarbon chain saturation, ion strength in suspension medium, and polar head type. To prevent crystallization and improve stability, sterols like cholesterol can be utilized as supplementary components. Therefore, it is crucial to carefully select the appropriate number and proportion of various types of lipids when determining liposome membrane performance.

Our Liposome Lipid Ratio Screening Services

We assist customers in advancing their liposome formulation development projects through the introduction of the following services.

Phospholipid type screening

The screening of phospholipid types is crucial for the preparation of liposomes, as phospholipids play a key role in their formation. Our scientists conduct studies to identify specific types of phospholipids that can enhance the stability and shelf life of liposomes by targeting the encapsulated active substances. For instance, we screen different types of phospholipids based on their degradation stability in water to improve the overall stability and rheology of the lipid bilayer.

Modification of phospholipids

Phospholipids, such as phosphatidylcholine (PC), phosphatidylethanolamine (PE), phosphatidylserine (PS), phosphatidylinositol (PI), phosphatidylglycerol (PG) and phosphatidic acid (PA). We offer modification services for both the non-polar and polar regions of these phospholipids, tailoring them to meet specific customer requirements. In addition, we have the capability to synthesize lipids including:

i. dipalmitoyl phosphatidylcholine (DPPC)
ii. dimyristoyl phosphatidylcholine (DMPC)
iii. distearyl phosphatidylcholine (DSPC)
iv. hydrogenated soy phosphatidylcholine (HSPC)
v. palmitoyl-2-oilyl-sn-glycerol-3-phosphate choline (POPC)
vi. 1,2-dioilyl-sn-glycerol-3-phosphate choline (DOPC)
vii. 1,2-distearyl-sn-glycerol-3-phosphate(1'-rac-glycerol) (DSPG)
viii. 1,2-dipalmitoyl-sn-glycerol-3-phosphate glycerol (DPPG)
ix. 1,2-distearyl-sn-glycerol-3-phosphate (DSPA)

Phospholipid ratio screening

The stability and permeability of liposomes are dependent on the phospholipid ratio in the formulation; thus, it is crucial to carefully screen for the appropriate phospholipid ratio. Moreover, a single lipid type often fails to meet the specific physical and chemical properties required for a particular system or adequately mimic the natural system it aims to replace or replicate. To address these challenges, our team has proposed complex lipid mixtures that synergistically combine multiple biological functions to fulfill customer project requirements.

Cholesterol ratio screening

Sterol lipids, including cholesterol (Chol) and its derivatives, are hydrophobic molecules that play a pivotal role in the structural integrity of animal cell membranes. Our research team conducts an investigation on lipid bilayers by incorporating Chol into them to explore parameters such as liposome fluidity, water permeability, and aggregation state. Ultimately, we seek to identify the optimal ratio for Chol addition.

Our Liposome Screening Process

Fig.1 Our workflow of liposome lipid ratio screening.Fig.1 The Workflow of Our Liposomal Lipid Ratio Screening Service. (CD Formulation)

Our Platform for Liposome Lipid Ratio Screening

Platform Specifics
Thin-film hydration
  • Simple operation
  • Under proper temperature and ultrasonic parameters, small uniform monolayer vesicles can be obtained.
Reverse evaporating method
  • This method can obtain a higher internal water phase loading capacity, so that the prepared liposomes have higher stability and are not easy to aggregate and precipitate, so the remaining solvent can be removed by dialysis, centrifugation and other methods.
Solvent injection method
  • This method can obtain a higher internal water phase loading capacity, so that the prepared liposomes have higher stability and are not easy to aggregate and precipitate, so the remaining solvent can be removed by dialysis, centrifugation and other methods.
Surfactant removal method
  • A gentle method of producing multiple types of vesicles and highly homogeneous liposomes.
Microfluidic technology
  • Multifunctional liposome preparation technology.
  • The lipid phase and the water phase pass through a channel with a diameter of tens to hundreds of microns at different entrances, and the lipid phase flow is focused into a narrow sheet under hydrodynamic action.
  • By adjusting the volume flow ratio of the water phase and the lipid phase, the length of the fluid channel, temperature, mixing conditions, and lipid concentration, variable liposome particle size (tens of nanometers to hundreds of microns) and narrow particle size distribution are achieved.

Our Advantages in Liposome Lipid Ratio Screening

  • State-of-the-art equipment and technology. Our cutting-edge equipment and advanced technology enable us to provide you with a comprehensive understanding of lipid properties.
  • Professional team. Our team consists of highly skilled scientists who possess extensive knowledge in lipid synthesis and modification, screening, and metabolomics for many years. This enables us to develop customized strategies to enhance the performance of liposomes.
  • Fast turnaround time. With our streamlined processes, we ensure swift turnaround times for the development of your liposome-based products, allowing you to achieve your goals promptly.

Published Data

Technology: dual asymmetric centrifugation technology application in liposome

Journal: European Journal of Pharmaceutical Sciences

IF: 9.2

Published: 2022

Results: In this study, the authors screened the effects of different membrane lipid compositions on DTX embedding (EE). Following initial screening studies using conventional probe ultrasound treatment devices to reduce the size of liposomes, further studies were conducted on liposomes prepared using the DAC method. The solubility of DTX liposomes corresponding to DTX-EE was determined by centrifugation of unencapsulated DTX. Liposome size, zeta potential (ZP) and polydispersion index (PDI) were also characterized.

Fig.2 Effects of different membrane lipid composition on DTX embedding.Fig.2 Effect study of different membrane lipid composition on DTX embedding.(Ann Mari Holsæter, et al., 2022)

At CD Formulation, our team of skilled formulation scientists specializes in conducting lipid ratio screening projects. Utilizing cutting-edge technology and state-of-the-art equipment, we are dedicated to delivering comprehensive and expert solutions for our valued clientele. If you have any inquiries, please do not hesitate to contact us.

References

  1. Ann Mari Holsæter, Kristina Wizgird, et al. How docetaxel entrapment, vesicle size, zeta potential and stability change with liposome composition – A formulation screening study. European Journal of Pharmaceutical Sciences, 2022, 10.
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