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Anticancer Drug‐Phospholipid Conjugate for Enhancement of Intracellular Drug Delivery
Author(s) -
Hwang Taewon,
Han Hee Dong,
Song Chung Kil,
Seong Hasoo,
Kim Jung Hyun,
Chen Xiaoyuan,
Shin Byung Cheol
Publication year - 2007
Publication title -
macromolecular symposia
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.257
H-Index - 76
eISSN - 1521-3900
pISSN - 1022-1360
DOI - 10.1002/masy.200750318
Subject(s) - liposome , conjugate , doxorubicin , in vivo , chemistry , drug delivery , phospholipid , flow cytometry , drug , endocytosis , drug carrier , pharmacology , biophysics , biochemistry , microbiology and biotechnology , chemotherapy , membrane , medicine , biology , cell , organic chemistry , mathematical analysis , mathematics , surgery
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 1 H‐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.