The drug loading method is a critical parameter for ensuring the quality of liposomes, and screening an appropriate drug loading method is a crucial step in the development of liposome formulations. The formulation development center at CD Formulation has played a pivotal role in facilitating the successful development of liposome formulations by our esteemed customers over the years, particularly excelling in drug loading method screening. Our team is equipped with state-of-the-art technology platforms and highly skilled scientists, making us your optimal choice for professional technical support.

The Importance of Liposome Drug Loading Method Screening

The release of liposomes is influenced by various factors, including particle size, composition of the phospholipid film, internal water phase, and drug delivery methods. Liposomal drug delivery methods can be categorized as active or passive. Passive drug delivery technology is commonly employed for lipid-soluble drugs, while active drug delivery technology is utilized for water-soluble drugs. Currently, the industrialization process of water-soluble drugs or amphiphilic drugs predominantly relies on active drug delivery methods to ensure optimal release and stability of liposome products. Therefore, selecting an appropriate drug delivery method remains a crucial factor in the development of liposomes.

Fig.1 The active and passive drug loading on the liposomes. (Nakhaei Pooria, et al. 2021)

Our Liposome Drug Loading Method Screening Services

At our state-of-the-art facility, we provide an array of services related to Liposome Drug Loading Method Screening. Our team of experts is dedicated to offering comprehensive solutions to help you optimize your drug delivery systems. We understand the importance of selecting the most suitable liposome drug loading method for your specific application, and thus, we strive to provide you with tailored services that address your unique needs.

Our services encompass a wide range of liposome drug loading methods, including the following:

Solubility study of main active ingredients

The research on drug characteristics involves the investigation of active substance stability, drug solubility, and HLB value. These factors play a crucial role in determining the appropriate method for drug loading. For example, lipid-soluble drugs are most suitable for passive drug loading technology, while water-soluble drugs are more suitable for active drug loading technology.

Comparison and screening of drug loading methods

The encapsulation of most drugs cannot be universally achieved through a single method; each drug necessitates a distinct approach to effectively manage its unique properties. For hydrophilic or amphiphilic drugs, by comparing different active drug loading methods (including pH gradient method, ammonium sulfate gradient method, and calcium acetate gradient method), the most effective drug loading method is systematically screened according to key parameters. In addition, the choice of active drug loading method needs to pay attention to dialysis demineralization technology. In view of the low incorporation efficiency of hydrophilic drugs, strategies are developed to increase the water phase in the core volume through different drug loading methods.

For fat-soluble substances, because there are many available technologies, and each technology has obvious advantages and disadvantages, according to different needs and final characterization results, the optimal selection of suitable drug loading methods should be paid attention to homogenization technology or dissolution residue in the later stage.

Our Platforms for Liposome Drug Loading Method Screening

Active Drug Loading Platforms

pH Gradient Technology By adjusting the pH of both the aqueous phase and the liposome, a sufficient transmembrane pH gradient is established across the lipid membrane. This gradient enables weak acid or weak alkali drugs to traverse the bilayer phospholipid membrane as molecules in the outer aqueous phase, while being encapsulated as ions within the inner aqueous phase of the lipid cavity.

Ammonium Sulfate Gradient Technology Ammonium sulfate buffer is used to prepare blank liposomes, and then ammonium sulfate in the aqueous phase outside the liposomes was removed by means of cross-flow dialysis, etc. Ammonium sulfate gradient is formed inside and outside the phospholipid membrane, and the drug is automatically loaded across the membrane under the condition of heating incubation.

Calcium Acetate Gradient Technology The blank liposome is prepared using calcium acetate, and subsequently the outer aqueous phase's calcium acetate is eliminated through methods such as dialysis, ultrafiltration, and ion exchange to establish a transmembrane concentration gradient of calcium acetate. As a result of the ionization and hydrolysis of calcium acetate, numerous acetic acid molecules (HAc) diffuse from the inner aqueous phase with higher concentration into the outer aqueous phase with lower concentration.

Passive Drug Loading Platforms

Reverse Evaporation Technology The technique involves the application of an oil-in-water emulsion or an inverse micelle, where lipids are present in the organic phase and the drug of interest is encapsulated within the aqueous phase, resulting in the formation of a bilayered liposome.

Thin-layer Dispersion Technology Lipids are mixed with solvents, then removed and a hydrophilic medium is added to form liposomes using ultrasound and membrane extrusion for uniform size distribution.

Solvent Injection Technology This technique involves dissolving phospholipid and cholesterol in ethanol or ether to create an organic phase, which is then injected into a water phase to form liposomes through the water-avoiding effect. The liposomes are subsequently purified by removing the organic solvent using rotary evaporation.

Double Emulsion Technology The key information in the given paragraph is about the process of obtaining a W/O/W emulsion by dissolving lipids in an organic solvent, adding water phase, and removing excess solvents.

Ultrasonication Disperse Technology Dissolving membrane material and lipid-soluble drug in organic solvent, removing the solvent through decompression, and treating the residual liquid with ultrasonic to remove unencapsulated drug.

Lyophilization Technology The preparation and shelf-life of lipid nanoparticles often result in the leakage of water-soluble drugs, leading to degradation caused by potential oxidation and other chemical reactions. These challenges significantly impede the commercial development of lipid nanoparticles. Freeze-drying technology offers a promising solution to overcome these issues.

Microfluidics Technology The microfluidic methods exhibit high versatility and flexibility, eliminating the need for post-production processing (such as extrusion or ultrasonic treatment) unlike traditional batch methods.

Supercritical Fluid Technology Supercritical fluid technology is used to prepare nanoparticles from pharmaceutical solutions through methods such as supercritical solution process (RESS), supercritical antisolvent method, and precipitation with compressed antisolvent (PCA).

Our Advantages in Liposome Drug Loading Method Screening

• Frontier technology. State-of-the-art equipment and cutting-edge technology enable us to provide detailed insights into your project.
• Professional team. Our team of experienced scientists specializes in studying drug lipid ratios, ensuring professional technical support.
• Efficient data processing and analysis. Benefit from our powerful data analysis center, which provides systematic and comprehensive data support for your project.

Published Data

The team at CD Formulation comprises of highly skilled formulation scientists specializing in liposome drug loading methods screening projects. Utilizing state-of-the-art equipment and cutting-edge technology, we are dedicated to delivering comprehensive and professional solutions for our esteemed clientele. If you have any inquiries, please do not hesitate to contact us.