IQUIR   05412
INSTITUTO DE QUIMICA ROSARIO
Unidad Ejecutora - UE
artículos
Título:
Stealth nanocarriers based sterosomes using PEG post-insertion process
Autor/es:
WAUTHOZ N.; BEJOUOD A. ; BENOIT J. ; CIES´LAK A.; LAUTRAM N.; LAFLEUR M. ; ORELLANA A.; GUILLAUME BASTIAT; HUREAUX J. ; SALOMON C.J.
Revista:
EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS
Editorial:
ELSEVIER SCIENCE BV
Referencias:
Lugar: Amsterdam; Año: 2017
ISSN:
0939-6411
Resumen:
Sterosomes (STEs), a new and promising non-phospholipidic liposome platform based on palmitic acid(PA) and cholesterol (Chol) mixtures, need to have polyethylene glycol (PEG) chains grafted to their surfacein order to obtain long-circulating nanocarriers in the blood stream. A post-insertion method waschosen to achieve this modification. The post-insertion process of PEG-modified distearoylphosphoethanolamine(DSPE-PEG) was monitored using the zeta potential value of STEs. Various conditionsincluding PEG chain length and the DSPE-PEG/PA-Chol ratio, were explored. Zeta potential of STEs changedfrom about 40 mV for non-modified STEs to values close to 0 mV by the end of the process, i.e. forPEG-modified STEs. The kinetics of DSPE-PEG insertion and the stability of the resulting PEG-modifiedSTEs were not considerably influenced, within the investigated range, by changes in PEG chain lengthsand in DSPE-PEG/PA-Chol proportion. The post-insertion of PEG chains reduced in vitro complement activationas well as in vitro macrophage uptake compared to the non-modified STEs. Moreover, longer bloodcirculation time in mice was established for PEG-modified STEs intravenously injected compared to nonmodifiedSTEs. These results establish that post-insertion process of PEG chains to STEs is a promisingstrategy for developing long-term circulating drug delivery nanocarriers.