The liposome development center at CD Formulation has been dedicated to exploring technologies and methodologies for enhancing the drug loading capacity and stability of liposomes for numerous years. Our team comprises experienced scientists proficient in liposome preparation, characterization, and application, providing customers with professional technical support and consultation services. Our research center has been providing extensive expertise in the field of lipid-to-lipid ratios for liposome-based drugs, assisting numerous clients with their research needs over the years.
In the preparation of liposomes, there may be instances where a low drug input leads to a drug loading efficiency exceeding 90%, or conversely, a high drug input results in a drug loading efficiency below 10%. Hence, accurately determining the actual drug-loading capacity of a liposome carrier is crucial as it represents the maximum amount of drug that can be loaded at a specific phospholipid concentration. The loading efficiency is typically expressed as the moles of drug per mole of phospholipid and calculated based on the molar fraction of captured drug (drug-lipid ratio or D/L ratio). The drug-to-lipid ratio (D/L ratio) is a critical process parameter that reflects the actual drug-loading capacity of liposomes and plays a pivotal role in optimizing each liposome formulation. It is closely associated with the encapsulation efficiency of liposomes. Generally, as the D/L ratio decreases, the amount of drug loaded into a single liposome decreases while facilitating easier encapsulation; conversely, higher D/L ratios result in increased administered drug doses, directly impacting therapeutic efficacy. The D/L ratio is influenced by factors such as composition, different biological materials, and loading methods; thus, increasing the D/L ratio can optimize liposome formulations. Furthermore, the D/L ratio can serve as an indicator for evaluating preparation methods' effectiveness by screening various ratios to analyze their effects on liposome integrity, pharmacodynamics, and other parameters.
Achieving optimal drug "load efficiency" during preparation and maintaining it throughout the life cycle of each liposome product, showing limited leakage in storage and systemic circulation, is key to obtaining the best therapeutically active liposome products. Our team of professionals is dedicated to providing you with the following research services to help you advance your liposome project more efficiently.
The drug to be loaded determines the loading method, as well as the D/L ratio. We provide services on property study of API including chemical structure, solubility parameters in liposome preparation media, etc.
The D/L ratio study helps clients predict and/or evaluate the "loading efficiency" and thus the actual effectiveness of the final liposome preformulation/formulation.
The D/L ratio plays an important role in the rational design and development of liposome formulations, which is a key parameter that must be studied for new liposome products. The effect of D/L ratio on the release spectrum of loaded drugs is studied to optimize the release parameters of liposomes in vitro.
Different liposome formulations are optimized and analyzed by studying the effects of D/L ratio on the whole life cycle of liposome drugs from development to production, from administration to clinical effect.
We evaluate the D/L ratio mainly by studying the possible interactions between drugs and lipids. For example, when cationic lipids usually interact with drugs with opposite charges, the D/L ratio will be affected, thus affecting the loading process and thus the loading efficiency of drugs.
The D/L ratio is determined by the type and proportion of lipids in the liposomes. By screening different lipid types, we aim to identify the optimal D/L ratio that ensures excellent drug load and release rate.
Fig.1 The workflow for studying liposome drug lipid ratios. (CD Formulation)
Platform | Specifics |
In vitro Release Platform | We provide this platform to help customers point the way to formulation optimization by studying the in vitro release properties of drugs in the effective D/L range. |
Stability Research Platform | At higher D/L values, drug crystals may destroy the liposomal bilayer. Capture is expected to decrease at higher D/L values, and the platform helps customers evaluate liposome formulations by studying the effects of drug to lipid ratios on stability. |
Technology: the drug-to-lipid ratio technique for regulating drug release
Journal: Journal of Liposome Research
IF: 4.4
Published: 2008
Results: In this study, the half-life of doxorubicin liposomes and the release properties of ciprofloxacin were studied by studying the D/L ratio and release relationship. Increasingly unusual disformations of adriamycin precipitate in the capsule were also observed. Linear crystals are observed at lower D/L values, however, as the D/L ratio increases, triangular and rectangular changes are observed and cause considerable distortion of vesicle morphology.
Fig.2 Cryo-transmission electron microscopy of doxorubicin liposomes at different drug-to-lipid ratios. (Johnston, M. J. W., et al., 2008)
The CD Formulation’s team is staffed by skilled formula scientists who specialize in lipid ratio screening projects. Utilizing cutting-edge technology and state-of-the-art equipment, we are committed to providing comprehensive and professional solutions to our valued customers. If you have any questions, please do not hesitate to contact us.
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