2012, Volume 14, Issue 8
Strategic Study of CAE >> 2012, Volume 14, Issue 8
Studies on preparation of folate-targeted boron liposomes as potential delivery agents for neutron capture therap
Beijing Friendship Hospital Affiliated to Capital Medical University, Beijing 100050, China
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Abstract
To prepare folate-targeted liposomes with high encapsulation efficiency is an effective targeted drug delivery agent for boron neutron capture therapy (BNCT). The double emulsion method is used to prepare liposomes. The combination of thin film hydration and ultrasonic dispersion method is used to prepare liposomes loaded with HBA,TBA or BBA. The content and the encapsulation efficiency of HBA,TBA or BBA liposomes are evaluated by high performance liquid chromatography (HPLC). As the basis of the encapsulation efficiency, the optimal conditions for preparing liposomes were explored by the single factor method. The optimal chromatographic conditions of the three drugs were filtered out. They had a good linear relation in a range of 1~100 μg/mL. The encapsulation efficiency of HBA, TBA and BBA liposomes were 25.7 %, 38.9 % and 94.8 % at the optimal preparation and condition. The optimal conditions for preparing BBA liposomes are as follows: the mass ratio of cholesterol and phospholipid is 1∶1, the ratio of drug and lipid is 1∶50 and the optimal pH value is 7.4. The entrapment efficiency for BBA liposomes in the optimal groups reached 94.8 %.The technique of preparing folate-targeted liposomes is feasible and the method of quality control is simple and high accuracy. Theliposomes appeare to be round, and well separated with high entrapment efficiency.
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