Long-Circulating, Temperature-Sensitive and EGFR-Targeted Liposomes for Drugs Delivery
Effectiveness of epidermal growth factor receptor(EGFR)-targeted, long circulating and temperature-sensitive liposomes(TSLs) is described using sterically stabilized gemcitabine-loaded liposomes in vitro. Development of long-circulating formulation of TSLs with the EGFR antibody attached was designed to expect an increase in binding and drug delivery efficiency to the target cells such as non-small cell lung cancer cells(A549) and human pancreatic carcinoma cells(PANC- 1). New TSLs were prepared using DPPC:DMPC:DSPC(4:1:1 molar ratio) by the REV method. Differential scanning calorimetry of TSLs showed the phase-transition around 402. Release of a self-quenching fluorescent probe, calcein, from TSLs was studied for evaluation of temperaturesensitivity. Anti-proliferation effect of gemcitabine-loaded TSLs and antibody-conjugated TSLs in A549 and PANC-1 were higher than free drug. We conclude that sterically stabilized immunoliposomes exhibited good stability, ability to recognize target cells, and higher potency. Further studies, including in vivo animal study, are under investigation.
Young-Ha Kim, Chong-Su Cho, Inn-Kyu Kang, Suk Young Kim and Oh Hyeong Kwon
S. K. Lim et al., "Long-Circulating, Temperature-Sensitive and EGFR-Targeted Liposomes for Drugs Delivery", Key Engineering Materials, Vols. 342-343, pp. 537-540, 2007