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

Li JM, Chen W, Wang H, Jin C, Yu XJ, Lu WY, Cui L, Fu DL, Ni QX, Hou HM - Acta Pharmacol. Sin. (2009)

Bottom Line: 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.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.

View Article: PubMed Central - PubMed

Affiliation: Pancreatic Disease Institute, Department of General Surgery, Huashan Hospital, Fudan University, Shanghai 200040, China.

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 drug-free 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.

Show MeSH

Related in: MedlinePlus

Inhibition rate-GEM concentration profile of 406 nm-GEM-NSP, 110 nm-GEM-NSP, GEM, and NSP on the human pancreatic cancer cell line BXPC-3 48 h (A) and 72 h (B) after administration in vitro. Significance of the difference between 406 nm-GEM-NSP and GEM. cP<0.005.
© Copyright Policy
Related In: Results  -  Collection


getmorefigures.php?uid=PMC4007180&req=5

fig4: Inhibition rate-GEM concentration profile of 406 nm-GEM-NSP, 110 nm-GEM-NSP, GEM, and NSP on the human pancreatic cancer cell line BXPC-3 48 h (A) and 72 h (B) after administration in vitro. Significance of the difference between 406 nm-GEM-NSP and GEM. cP<0.005.

Mentions: The cytotoxicity of 110 nm-GEM-NSPs and 406 nm-GEM-NSPs on BXPC-3 cells 48 and 72 h after administration was detected by the MTT assay (Figure 4). The inhibition rate-administered concentration profiles of 406 nm-GEM-NSPs, 110 nm-GEM-NSPs, and GEM were all higher than those of NSPs alone (P<0.05). The inhibition rate of blank NSPs was about 20% with good cell morphology, without obvious correlation with time or concentration, which indicated that NSPs had good biocompatibility, without obvious cytotoxicity (grade 1–2), according to the United States Pharmacopeia (USP 28 )35.


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

Li JM, Chen W, Wang H, Jin C, Yu XJ, Lu WY, Cui L, Fu DL, Ni QX, Hou HM - Acta Pharmacol. Sin. (2009)

Inhibition rate-GEM concentration profile of 406 nm-GEM-NSP, 110 nm-GEM-NSP, GEM, and NSP on the human pancreatic cancer cell line BXPC-3 48 h (A) and 72 h (B) after administration in vitro. Significance of the difference between 406 nm-GEM-NSP and GEM. cP<0.005.
© Copyright Policy
Related In: Results  -  Collection

Show All Figures
getmorefigures.php?uid=PMC4007180&req=5

fig4: Inhibition rate-GEM concentration profile of 406 nm-GEM-NSP, 110 nm-GEM-NSP, GEM, and NSP on the human pancreatic cancer cell line BXPC-3 48 h (A) and 72 h (B) after administration in vitro. Significance of the difference between 406 nm-GEM-NSP and GEM. cP<0.005.
Mentions: The cytotoxicity of 110 nm-GEM-NSPs and 406 nm-GEM-NSPs on BXPC-3 cells 48 and 72 h after administration was detected by the MTT assay (Figure 4). The inhibition rate-administered concentration profiles of 406 nm-GEM-NSPs, 110 nm-GEM-NSPs, and GEM were all higher than those of NSPs alone (P<0.05). The inhibition rate of blank NSPs was about 20% with good cell morphology, without obvious correlation with time or concentration, which indicated that NSPs had good biocompatibility, without obvious cytotoxicity (grade 1–2), according to the United States Pharmacopeia (USP 28 )35.

Bottom Line: 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.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.

View Article: PubMed Central - PubMed

Affiliation: Pancreatic Disease Institute, Department of General Surgery, Huashan Hospital, Fudan University, Shanghai 200040, China.

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 drug-free 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.

Show MeSH
Related in: MedlinePlus