John Garner

PLGA-PEG-COOH from PolySciTech used in development of nanoparticle-based anticoagulant (Alteplase) delivery system for treatment of blood clotting

Blog Post created by John Garner on Apr 11, 2019

Perez, 2019 alteplase delivery system polyscitech PLGA-PEG-COOH.jpg

The formation of blood-clots within the human blood system is part of several severe diseases including heart-attack and stroke. Alteplase is a is a tissue plasminogen activator which acts to break up these clots. To improve the efficiency and specificity of this action, the Alteplase can be encapsulated in nanoparticles decorated with a plaque-homing peptide, CREKA, which binds to fibrin-fibronectin clots and accumulates at the surface of plaques. Recently, Researchers at Universidad de Sevilla (Spain) used PLGA-PEG-COOH (AI034) from PolySciTech ( to develop drug-delivery nanoparticles carrying Alteplase. This research holds promise to provide for improved treatments of diseases associated with clotting such as stroke and heart-attacks. Read more: Fernández Pérez, Irene. "Estudio preliminar de una formulación de Nanoparticulaspara targetactivo de un." Thesis Presentation Universidad de Sevilla (2018). %C3%A9rez.pdf?sequence=1


“Abstract [*translated*]: The present work fits into the currently emerging field of nanomedicine. Specifically, it is a preliminary study based in the design and development of nanoparticles that will serve as a system of administration of a fibrinolytic drug, which is intended to actively address the pathological thrombi formed by the process of blood coagulation. To do this, several batches of PLGA nanoparticles have been synthesized using different polymers (Resomer® 504H and PLGA-PEG) and varying amounts/concentration of drug (Actilyse®). Nanoparticle synthesis has been carried out by the double emulsion method with evaporation of solvent, obtaining particles of an adequate nanometric size (~ 200 - 300 nm) with narrow size distribution and negative zeta potential. The tests carried out on the efficacy of drug encapsulation presented good results. The maximum loading efficiency (97%) was observed for PLGA-PEG particles loaded at 5% w / w (active / polymer). To carry out the preliminary study of the design of these nanoparticles for the targeting of clots, the CREKA pentapeptide was used for surface functionalization of the particles. This enables a process of bioconjugation. This lead to a slight increase in the average size of the particles and in the PdI values. The surface load data obtained showed a potentially better conjugation efficiency for the PLGA-PEG particles. However, this bioconjugation data is very preliminary.”


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