Journal
BIOMATERIALS
Volume 30, Issue 29, Pages 5751-5756Publisher
ELSEVIER SCI LTD
DOI: 10.1016/j.biomaterials.2009.07.021
Keywords
Tissue plasminogen activator; Half-life; Prolong; Liposomes; PEG; Fibrinolysis
Funding
- Ministry of Education and Human Resources Development (MOE)
- Ministry of Commerce, Industry and Energy (MOCIE)
- Ministry of Labor (MOLAB) through the fostering project of the Lab of Excellency
- National Research Foundation of Korea [과09B2106] Funding Source: Korea Institute of Science & Technology Information (KISTI), National Science & Technology Information Service (NTIS)
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Tissue plasminogen activator (tPA), a widely used thrombolytic agent, has an application limit due to short half-life. To prolong the half-life of tPA, liposomes composed of egg phosphatidylcholine (EPC), cholesterol (CHOL) and sodium cholesterol-3-sulfate (CS) were prepared by lipid film method. In addition, distearolyphosphatidyl ethanolamine-N-poly(ethylene glycol) 2000 (DSPE-PEG 2000) was included to give steric barrier to liposomes. Physicochemical characteristics such as particle size, zeta potential, entrapment efficiency and long-term storage stability at 4 degrees C were investigated. The fibrinolytic activity of tPA-loaded in liposomes was confirmed by fibrin clot lysis assay. In vivo pharmacokinetic properties of tPA and the effect of PEG on the blood circulation of tPA-loaded in liposomes in circulation were also evaluated. Both conventional liposomes (EPCL) and PEGylated liposomes (EPC-PEGL) were proper as an injectable formulation with small particle size. Loading process of tPA into liposomes did not alter fibrinolytic activity of intact tPA. Encapsulation of tPA into EPCL and EPC-PEGL prolonged half-life of tPA by 16 and 21 folds compared with free tPA, respectively. Therefore, the use of liposomes could prolong the circulation lifetimes and longevity effect of liposomes on tPA was increased by PEG. (C) 2009 Elsevier Ltd. All rights reserved.
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