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Li, L.* ; ten Hagen, T.L.M.* ; Schipper, D.* ; Wijnberg, T.M.* ; van Rhoon, G.C.* ; Eggermont, A.M.M.* ; Lindner, L.H. ; Koning, G.A.*

Triggered content release from optimized stealth thermosensitive liposomes using mild hyperthermia.

J. Control. Release 143, 274-279 (2010)
DOI PMC
Open Access Green möglich sobald Postprint bei der ZB eingereicht worden ist.
Liposomes are potent nanocarriers to deliver chemotherapeutic drugs to tumors. However, the inefficient drug release hinders their application. Thermosensitive liposomes (TSL) can release drugs upon heat. This study aims to identify the optimum 1,2-distearoyl-sn-glycero-3-phosphoethanolamine-N-PEG(2000) (DSPE-PEG(2000)) concentration in stealth TSL to improve content release efficiency under mild hyperthermia (HT). TSL were prepared with DSPE-PEG2000 from 1 to 10 mol%, around 80 nm in size. Quenched carboxyfluorescein (CF) in aqueous phase represented encapsulated drugs. In vitro temperature/time-dependent CF release and TSL stability in serum were quantified by fluorometry. In vivo CF release in dorsal skin flap window chamber models implanted with human BLM melanoma was captured by confocal microscopy. In vitro heat triggered CF release increased with increasing DSPE-PEG2000 density. However, 6 mol% and higher DSPE-PEG2000 caused CF leakage at physiological temperature. TSL with 5 mol% DSPE-PEG2000 were stable at 37 degrees C. while released 60% CF in 1 min and almost 100% CF in 1 h at 42 degrees C. In vivo optical intravital imaging showed immediate massive CF release above 41 degrees C. In conclusion, incorporation of 5 mol% DSPE-PEG(2000) optimized stealth TSL content release triggered by HT.
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Publikationstyp Artikel: Journalartikel
Dokumenttyp Wissenschaftlicher Artikel
Korrespondenzautor
Schlagwörter Thermosensitive liposomes; Hyperthermia; Poly(ethylene glycol); Drug delivery; Triggered release; Tumor; Intravital microscopy; STERICALLY STABILIZED LIPOSOMES; TEMPERATURE-SENSITIVE LIPOSOMES; PROLONGED CIRCULATION TIME; HUMAN TUMOR XENOGRAFT; POLYETHYLENE-GLYCOL; VASCULAR-PERMEABILITY; PHASE-TRANSITION; POLY(ETHYLENE GLYCOL); ANTITUMOR-ACTIVITY; IN-VITRO
ISSN (print) / ISBN 0168-3659
e-ISSN 1873-4995
Zeitschrift Journal of Controlled Release
Quellenangaben Band: 143, Heft: 2, Seiten: 274-279 Artikelnummer: , Supplement: ,
Verlag Elsevier
Verlagsort Amsterdam
Nichtpatentliteratur Publikationen
Begutachtungsstatus Peer reviewed
Institut(e) CCG Tumor Therapy with Hyperthermia (IMI-KTH)