The liposome analysis center of CD Formulation has been assisting customers from diverse backgrounds in efficiently evaluating the quality of liposomes for many years. With extensive project experience in detecting liposome encapsulation rates, we are well-equipped to provide professional support and comprehensive analysis and testing services throughout the entire R&D process and even the complete life cycle of liposomes.
Encapsulation efficiency is a critical quality attribute of liposomes, referring to the percentage of drug content encapsulated within the lipid bilayer relative to the total dose. This parameter reflects the degree of drug encapsulation in liposomes and guides improvements in preparation processes. Encapsulation efficiency serves as an essential indicator for evaluating preparation processes and assessing liposome quality, enabling high efficacy and low toxicity while improving therapeutic indices, reducing adverse reactions, and minimizing required dosages compared with conventional preparations.
Due to the distinct characteristics of the encapsulated drug and the diverse liposome membrane materials, determining the optimal method for assessing the encapsulation rate of each liposome often necessitates experimental investigation. The pivotal aspect in determining this rate lies in effectively segregating the encapsulated drug from its unencapsulated counterpart, followed by employing spectroscopy, chromatography, and other analytical techniques to quantify their respective concentrations. Techniques employed for evaluating encapsulation rates encompass centrifugation, ultrafiltration centrifugation, dextran gel column method, microcolumn centrifugation, dialysis and reverse dialysis methods, protamine agglutination method, fluorescence method, among others.
The decision tree for selecting the measurement method for liposome encapsulation rate is summarized based on the properties of the substance under test and the characteristics of various measurement methods.
Fig.1 Decision tree for the selection of methods to determine liposome encapsulation efficiency. (CD Formulation)
The encapsulation efficiency of liposomes is influenced by various factors, such as the composition and length of the phospholipid chain in the liposome membrane, its charge, particle size, preparation method, and the nature of the drug being encapsulated. By focusing on improving one or several of these factors, we help clients to enhance or increase the encapsulation efficiency of liposomes.
a. Lipid Membrane Composition and Liposome Potential. By investigating the lipid bilayer membrane composition, we aim to examine the impact of composition on drug distribution within the membrane and encapsulation rate, with the ultimate goal of optimizing lipid formulation composition for enhanced encapsulation efficiency.
b. Study on API Properties. Factors, such as the solubility of the API itself, the polarity and the matching degree of the bilayer, will affect the encapsulation rate. Drawing on our expertise, drugs with high lipophilicity or high hydrophilicity, that is, drugs with lgPoct in 4.5-0.3, can form liposomes with high encapsulation rate. We can modify the API to improve the encapsulation rate or stability of the liposomes, such as salinization or esterification.
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Technology: differential scanning calorimetry technique to determine EE%
Journal: Journal of Thermal Analysis and Calorimetry
IF: 4.4
Published: 2017
Results: In this study, a new method was proposed to detect the encapsulation rate by differential scanning calorimetry (DSC). The effect of increasing the concentration of free base on the bilayer membrane was determined according to the size, polydispersion index, zeta potential, encapsulation efficiency (EE%) and partition coefficient.
The CD Formulation team possesses extensive project experience in liposome encapsulation assay. We employ a unique technology selection strategy and adopt a systematic project management approach to ensure the delivery of professional data and analysis results to our esteemed customers. For further information, please feel free to contact us.
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