TY - JOUR
T1 - Anticancer drug-phospholipid conjugate for enhancement of intracellular drug delivery
AU - Hwang, Taewon
AU - Han, Hee Dong
AU - Song, Chung Kil
AU - Seong, Hasoo
AU - Kim, Jung Hyun
AU - Chen, Xiaoyuan
AU - Shin, Byung Cheol
PY - 2007
Y1 - 2007
N2 - The Molecular Imaging Program at Stanford (MIPS), Department of Radiology and Bio-X Program, Stanford University School of Medicine, 1201 Welch Rd, P095, Stanford, CA 9430505484, USA 10.1002/masy.200750318 Tumor specific delivery of anti-cancer drugs is one of the major challenges faced by drug development processes. In this study, we prepared a doxorubicin (DOX)-conjugated liposome (DCL) by incorporating the newly synthesized DSPE-PEG2000-DOX (DPD) into liposomes as a lipid component and tested its anti-tumor activity in vivo. DPD was synthesized by coupling DOX to DSPE-PEG2000-COOH via amide linkage and the chemical structure of resulting DPD was confirmed by 1H-NMR analysis. DCL having liposome size of 130 nm was prepared through thin film cast-hydration method. DCL was found to have significantly higher cellular uptake than conventional liposomes as confirmed by flow cytometry analysis. Anti-tumor activity of DCL against murine B16F10 melanoma tumor-bearing mice revealed that DCL inhibits tumor growth more efficiently than the conventional liposomes, presumably attributed to DOX mediated endocytosis process.
AB - The Molecular Imaging Program at Stanford (MIPS), Department of Radiology and Bio-X Program, Stanford University School of Medicine, 1201 Welch Rd, P095, Stanford, CA 9430505484, USA 10.1002/masy.200750318 Tumor specific delivery of anti-cancer drugs is one of the major challenges faced by drug development processes. In this study, we prepared a doxorubicin (DOX)-conjugated liposome (DCL) by incorporating the newly synthesized DSPE-PEG2000-DOX (DPD) into liposomes as a lipid component and tested its anti-tumor activity in vivo. DPD was synthesized by coupling DOX to DSPE-PEG2000-COOH via amide linkage and the chemical structure of resulting DPD was confirmed by 1H-NMR analysis. DCL having liposome size of 130 nm was prepared through thin film cast-hydration method. DCL was found to have significantly higher cellular uptake than conventional liposomes as confirmed by flow cytometry analysis. Anti-tumor activity of DCL against murine B16F10 melanoma tumor-bearing mice revealed that DCL inhibits tumor growth more efficiently than the conventional liposomes, presumably attributed to DOX mediated endocytosis process.
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U2 - 10.1002/masy.200750318
DO - 10.1002/masy.200750318
M3 - Article
AN - SCOPUS:34547169978
SN - 1022-1360
VL - 249-250
SP - 109
EP - 115
JO - Macromolecular Symposia
JF - Macromolecular Symposia
ER -
