Please use this identifier to cite or link to this item: https://doi.org/10.1002/jps.21988
Title: The functional roles of poly(ethylene glycol)-lipid and lysolipid in the drug retention and release from lysolipid-containing thermosensitive liposomes in vitro and in vivo
Authors: Banno, B.
Ickenstein, L.M.
Chiu, G.N.C. 
Bally, M.B.
Thewalt, J.
Brief, E.
Wasan, E.K.
Keywords: Drug release assay
Lysolipid
Micelles
Peg-lipid
Pharmacokinetics
Poly(ethylene glycol)
Thermosensitive liposomes
Issue Date: May-2010
Citation: Banno, B., Ickenstein, L.M., Chiu, G.N.C., Bally, M.B., Thewalt, J., Brief, E., Wasan, E.K. (2010-05). The functional roles of poly(ethylene glycol)-lipid and lysolipid in the drug retention and release from lysolipid-containing thermosensitive liposomes in vitro and in vivo. Journal of Pharmaceutical Sciences 99 (5) : 2295-2308. ScholarBank@NUS Repository. https://doi.org/10.1002/jps.21988
Abstract: Triggered release of liposomal contents following tumor accumulation and mild local heating is pursued as a means of improving the therapeutic index of chemotherapeutic drugs. Lysolipid-containing thermosensitive liposomes (LTSLs) are composed of dipalmitoylphosphatidylcholine (DPPC), the lysolipid monostearoylphosphatidylcholine (MSPC), and poly(ethylene glycol)-conjugated distearoylphosphatidylethanolamine (DSPE-PEG2000). We investigated the roles of DSPE-PEG2000 and lysolipid in the functional performance of the LTSL-doxorubicin formulation. Varying PEG-lipid concentration (0-5 mol%) or bilayer orientation did not affect the release; however, lysolipid (0-10 mol%) had a concentration-dependent effect on drug release at 42°C in vitro. Pharmacokinetics of various LTSL formulations were compared in mice with body temperature controlled at 37°C. As expected, incorporation of the PEG-lipid increased doxorubicin plasma half-life; however, PEG-lipid orientation (bilayer vs. external leaflet) did not significantly improve circulation lifetime or drug retention in LTSL. Approximately 70% of lysolipid was lost within 1 h postinjection of LTSL, which could be due to interactions with the large membrane pool of the biological milieu. Considering that the present LTSL-doxorubicin formulation exhibits significant therapeutic activity when used in conjunction with mild heating, our current study provided critical insights into how the physicochemical properties of LTSL can be tailored to achieve better therapeutic activity. © 2009 Wiley-Liss, Inc. and the American Pharmacists Association.
Source Title: Journal of Pharmaceutical Sciences
URI: http://scholarbank.nus.edu.sg/handle/10635/106430
ISSN: 00223549
DOI: 10.1002/jps.21988
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