Preparation of albumin nanospheres loaded with gemcitabine and their cytotoxicity against BXPC-3 cells in vitro.
OBJECTIVE
To optimize formulation methods for loading gemcitabine (GEM), the main drug against pancreatic cancer, into albumin nanoparticles for extended blood circulation and improved efficacy.


METHODS
GEM was loaded into two sizes of disolvation-crosslinked bovine serum albumin nanoparticles, with a mean diameter of 109.7 nm and 405.6 nm, respectively, by co-precipitation (the direct method) and follow-up adsorption (the indirect method). The antitumor activities of the two nanoparticulate formulations, were evaluated according to their anti-proliferative effects on the human pancreatic cell line BXPC-3, which were assessed using the MTT assay.


RESULTS
The two nanoparticulate formulations, created by direct co-precipitation and indirect adsorption, possessed smooth surfaces and high drug loading efficiencies, 83% and 93% at 11% and 13% drug loading, respectively. The two formulations released GEM for 8 and 12 h, respectively, and significantly improved anti-BXPC-3 proliferation effects, as compared with the GEM solution and the drug-free albumin particles.


CONCLUSIONS
Co-precipitating and adsorbing GEM into albumin particles resulted in sustained-release nanoparticulate formulations with improved antitumor cytotoxicity. The result suggests that this is a useful formulation strategy for improving the antitumor efficacy of GEM.
Li
Jin-ming
JM
Pancreatic Disease Institute, Department of General Surgery, Huashan Hospital, Fudan University, Shanghai 200040, China.
Chen
Wei
W
Wang
Hao
H
Jin
Chen
C
Yu
Xian-jun
XJ
Lu
Wei-yue
WY
Cui
Long
L
Fu
De-liang
DL
Ni
Quan-xing
QX
Hou
Hui-min
HM
D000964:Antimetabolites, Antineoplastic / Q000008:administration & dosage* / Q000627:therapeutic use; D003841:Deoxycytidine / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000627:therapeutic use; D004337:Drug Carriers / Q000627:therapeutic use*; D006801:Humans; D053769:Nanocapsules / Q000627:therapeutic use*; D054118:Nanospheres / Q000627:therapeutic use*; D010190:Pancreatic Neoplasms / Q000188:drug therapy*; D012710:Serum Albumin, Bovine / Q000378:metabolism; D014407:Tumor Cells, Cultured; D000093542:Gemcitabine
D000964:Antimetabolites, Antineoplastic; D004337:Drug Carriers; D053769:Nanocapsules; D003841:Deoxycytidine; D012710:Serum Albumin, Bovine; D000093542:Gemcitabine