TY - JOUR
T1 - Anti-tumor activity of liposomal glucocorticoids: The relevance of liposome-mediated drug delivery, intratumoral localization and systemic activity
AU - Kluza, Ewelina
AU - Yeo, Sin Yuin
AU - Schmid, Sophie
AU - Van der Schaft, Daisy W. J.
AU - Boekhoven, Renate W.
AU - Schiffelers, Raymond M.
AU - Storm, Gert
AU - Strijkers, Gustav J.
AU - Nicolay, Klaas
PY - 2011/4/10
Y1 - 2011/4/10
N2 - Tumor-associated inflammation has been recognized as an important tumor growth propagator and, therefore, represents an attractive target for anti-cancer therapy. In the current study, inspired by recent findings on the anti-tumor activity of liposomal glucocorticoids, we introduce paramagnetic and fluorescent liposomes, encapsulating prednisolone phosphate (PLP), to evaluate the local delivery of liposomal glucocorticoids to the tumor and its importance for the therapeutic response. The new multifunctional liposomes (Gd-PLP-L) (120nm diameter, 5.8mg PLP/60?mol lipid, bioexponential blood-clearance kinetics (T(1/2?)=2.4?0.5h, T(1/2?)=42.0?12.4h), drug leakage of 15%/72h (in vitro)), containing 25mol% Gd-DTPA-lipid and 0.1mol% of rhodamine-lipid, were tested in B16F10 melanoma subcutaneously inoculated in C57BL/6 mice, and compared to the original PLP formulation (PLP-L). A single dose of Gd-PLP-L (20mgPLP/kg/week, i.v.) was found to significantly inhibit tumor growth compared to non-treated mice (P
AB - Tumor-associated inflammation has been recognized as an important tumor growth propagator and, therefore, represents an attractive target for anti-cancer therapy. In the current study, inspired by recent findings on the anti-tumor activity of liposomal glucocorticoids, we introduce paramagnetic and fluorescent liposomes, encapsulating prednisolone phosphate (PLP), to evaluate the local delivery of liposomal glucocorticoids to the tumor and its importance for the therapeutic response. The new multifunctional liposomes (Gd-PLP-L) (120nm diameter, 5.8mg PLP/60?mol lipid, bioexponential blood-clearance kinetics (T(1/2?)=2.4?0.5h, T(1/2?)=42.0?12.4h), drug leakage of 15%/72h (in vitro)), containing 25mol% Gd-DTPA-lipid and 0.1mol% of rhodamine-lipid, were tested in B16F10 melanoma subcutaneously inoculated in C57BL/6 mice, and compared to the original PLP formulation (PLP-L). A single dose of Gd-PLP-L (20mgPLP/kg/week, i.v.) was found to significantly inhibit tumor growth compared to non-treated mice (P
KW - Anti-tumor therapy
KW - Tumor-associated inflammation
KW - Multifunctional liposomes
KW - Magnetic resonance imaging
KW - Monitoring of drug delivery
U2 - 10.1016/j.jconrel.2010.11.031
DO - 10.1016/j.jconrel.2010.11.031
M3 - Article
C2 - 21130819
SN - 0168-3659
VL - 151
SP - 10
EP - 17
JO - Journal of Controlled Release
JF - Journal of Controlled Release
IS - 1
ER -