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Preparation of thermosensitive magnetic liposome encapsulated recombinant tissue plasminogen activator for targeted thrombolysis

Abstract Recombinant tissue plasminogen activator (rtPA) was encapsulated in thermosensitive magnetic liposome (TML) prepared from 1,2-dipalmitoyl- sn -glycero-3-phosphocholine, distearolyphosphatidyl ethanolamine- N -poly(ethylene glycol) 2000, cholesterol and Fe 3 O 4… Click to show full abstract

Abstract Recombinant tissue plasminogen activator (rtPA) was encapsulated in thermosensitive magnetic liposome (TML) prepared from 1,2-dipalmitoyl- sn -glycero-3-phosphocholine, distearolyphosphatidyl ethanolamine- N -poly(ethylene glycol) 2000, cholesterol and Fe 3 O 4 magnetic nanoparticles by solvent evaporation/sonication and freeze-thaw cycles method. Response surface methodology was proved to be a powerful tool to predict the drug encapsulation efficiency and temperature-sensitive drug release. Validation experiments verified the accuracy of the model that provides a simple and effective method for fabricating TML with controllable encapsulation efficiency and predictable temperature-sensitive drug release behavior. The prepared samples were characterized for physico-chemical properties by dynamic light scattering, transmission electron microscopy, X-ray diffraction and differential scanning calorimetry. Temperature-sensitive release of rtPA could be confirmed from in vitro thrombolysis experiments. A thrombolytic drug delivery system using TML could be proposed for magnetic targeted delivery of rtPA to the site of thrombus followed by temperature-triggered controlled drug release in an alternating magnetic field.

Keywords: magnetic liposome; drug; thermosensitive magnetic; recombinant tissue; plasminogen activator; tissue plasminogen

Journal Title: Journal of Magnetism and Magnetic Materials
Year Published: 2017

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