Preparation of albumin nanospheres loaded with gemcitabine and their cytotoxicity against BXPC-3 cells in vitro

Abstract

Aim: 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 drugfree albumin particles. Conclusion: 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.

Formulation and evaluation of gemcitabine-loaded solid lipid nanoparticles

“…This is attributed by the higher phagocytotic rates for the uptake of nanoparticles in liver and spleen, than cells of other tissues. A similar phenomenon was observed in the selective targeting of albumin nanospheres (Li et al, 2009). The results of stability testing revealed that there was no significant change in the mean Figure 2.…”

“…Gemcitabine represents an advance in pancreatic cancer care. The major limitation of gemcitabine is short half life and strong side effects when administered intravenously (Li et al, 2009;Jia et al, 2010). Short half lives are commonly due to fast renal clearance, decreased protein binding and enzymatic degradation (Werle & Bemkop Schnurch, 2006).…”

RGD-conjugated albumin nanoparticles as a novel delivery vehicle in pancreatic cancer therapy

“…The albumin nanoparticles were prepared by the desolvation-crosslinking technique as previously described. 26 Briefly, 10 ml aqueous BSA (2.5% w/v) was prepared. The pH was adjusted to 8.0-8.2 with NaOH (1 mol/L).…”

An in vitro and in vivo study of gemcitabine-loaded albumin nanoparticles in a pancreatic cancer cell line

“…We have previously reported on the use of albumin nanoparticles as drug carriers to encapsulate Gem in pancreatic cancer, [26][27][28] in which two sizes of Gem-loaded albumin nanoparticles (110 nm and 406 nm) were successfully prepared. Both indicated improved antitumor cytotoxicity and prolonged drug release characteristics.…”