Cytotoxic effects of Gemcitabine-loaded liposomes in human anaplastic thyroid carcinoma cells

Celano, Marilena; Calvagno, Maria Grazia; Bulotta, Stefania; Paolino, Donatella; Arturi, Franco; Rotiroti, D.; Fresta, Massimo; Russo, Diego

doi:10.1186/1471-2407-4-63

Cited by 85 publications

(66 citation statements)

References 22 publications

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“…The time for slow release of GEM from GEM-NSPs observed in this study was not longer than 12 h, probably because of GEM high water solubility, as reported previously [13][14][15][16][17][18][19] . However, since pure GEM is rapidly metabolized, prolongation of the release time of GEM by GEM-NSPs represents an improvement.…”

Section: Discussionsupporting

confidence: 82%

“…Drug loadings were 11.25% and 13.40%; drug encapsulation rates were 82.92% and 92.56%, respectively. These parameters were somewhat higher than in other kinds of drug-loaded nanoparticles prepared analogously [13][14][15][16][17][18][19] . Zeta potentials were -24.4 and -15.6 mV, respec- Figure 1).…”

Section: Characterization Of Gem-nspsmentioning

confidence: 78%

“…Albumin is a safe, nontoxic, biocompatible, and biodegradable water-soluble protein present in human plasma [10][11][12] . No problems with hemolysis or immunogenicity have been associated with albumin, in contrast to artificial npg materials such as polycaprolactone, polycyanoacrylate, or polybutylcyanoacrylate [13][14][15][16][17][18][19] . Although these compounds are also biodegradable, their safety following intravenous injection has not been confirmed.…”

Section: Introductionmentioning

confidence: 99%

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

Chen

Wang

et al. 2009

Acta Pharmacol Sin

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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.

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Section: Discussionsupporting

confidence: 82%

Section: Characterization Of Gem-nspsmentioning

confidence: 78%

Section: Introductionmentioning

confidence: 99%

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

Chen

Wang

et al. 2009

Acta Pharmacol Sin

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“…For this reason, a liposome formulation of Si 34 was prepared and proposed as a possible drug carrier for both in vitro and in vivo applications. Our previous results (Celano et al 2004, Calvagno et al 2007 showed that the liposomal carrier may provide even in vitro effective advantages over free drugs in terms of both dosedependent and exposition time-dependent anticancer effect. In the perspective of a possible in vivo application, pegylated liposomes were prepared and, hence, the presence of polyethylene glycol (PEG) moieties on the surface of liposomes may promote the carrier bioadhesion at the level of cellular surface, thus stimulating a liposome-cell interaction (Sadzuka & Hirota 1998, Sadzuka et al 2003, i.e., liposome uptake into tumor cells, inter-membrane drug passage, and/or microenvironments with high local drug concentrations that favor intracellular drug entrance (Calvagno et al 2007).…”

Section: Discussionmentioning

confidence: 99%

Cytotoxic effects of a novel pyrazolopyrimidine derivative entrapped in liposomes in anaplastic thyroid cancer cells in vitro and in xenograft tumors in vivo

Celano¹,

Schenone²,

Cosco³

et al. 2008

Endocrine Related Cancer

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In this study, we evaluated the activity of two novel pyrazolopyrimidine derivatives (Si 34 and Si 35) against ARO cells, a human anaplastic thyroid cancer cell line. ARO cells exposed to different concentrations of the drugs showed a reduced growth rate and an increase of mortality. After 72 h incubation, doses of 5 and 10 mM Si 34 determined a decrease of cell counts by w25% and w75% compared with those of control cells respectively. Similar findings were observed using Si 35. Treatment with both Si 34 and Si 35 at 10 mM increased cell mortality also (w29% and w18% respectively). At these concentrations, a decrease in cyclin D1 levels was observed. To improve the biopharmaceutical properties, a liposome formulation was prepared. When entrapped in unilamellar liposomes, Si 34 exerted its cytotoxic effects even at lower doses (maximal inhibition at 5 mM) and after shorter incubation time (48 h) either in ARO or other thyroid cancer cell lines. The effects were associated with weak apoptotic death. Inhibition of epidermal growth factorstimulated src and ERK phosphorylation, as well as reduction of migration properties of ARO cells was also observed. Moreover, the growth of tumor xenografts induced in severe combined immunodeficiency (SCID) mice was inhibited by i.v. administration of 25-50 mg/kg of the drug liposomal formulation. In conclusion, the liposomal preparation of this novel pyrazolopyrimidine derivative appears to be a promising tool for the treatment of anaplasic thyroid cancer.

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“…Recently, a wide range of different types of drug delivery systems have been investigated, including liposomes, polymers, dendrimers, molecular conjugates, etc. [8][9][10][11] However, the safety issue of these artificial materials remains unknown. Albumin is a safe, nontoxic, biocompatible and biodegradable water-soluble protein present in human plasma and is being widely used clinically, which makes it an ideal candidate for drug delivery vehicle.…”

Section: Introductionmentioning

confidence: 99%

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

Zhang

et al. 2012

Cancer Biology & Therapy

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These authors contributed equally to this work. Keywords: nanoparticles, albumin, RGD, FITC, delivery, pancreatic cancer, therapyIntegrin avb3 receptor is expressed on several types of cancer cells, including pancreatic cancer cells, and plays an important role in tumor growth and metastasis. The ability to target the integrin avb3 receptor on cancer cells increases the efficacy of targeted therapy and reduces the side effects. The aim of this study is to develop a novel arginine-glycineaspartic acid (RGD) peptide-conjugated albumin nanoparticle to enhance the intracellular uptake of anticancer drug into the pancreatic cancer cells through receptor-mediated endocytosis. In cellular uptake studies, the fluorescent signal of RGD-conjugated BSANPs in BxPC3 cells was higher than that of BSANPs without RGD conjugation as determined by fluorescence spectrophotometer. We also found that BSANPs bound to BxPC3 cells in a time-and concentration-dependent manner. The uptake of RGD-conjugated BSANPs by pancreatic cancer cells was inhibited by an excess amount of free RGD peptide, indicating that the binding and/or uptake were mediated by the avb3 receptor. Furthermore, the nanoparticles were found to be located close to the nuclei by using laser scanning confocal microscopy. Besides, no significant in vitro cytotoxicity was observed as measured with MTT assay. Both in vitro and in vivo antitumor efficacy was improved by targeting gemcitabine-loaded nanoparticles to BxPC-3 cells using RGD peptides. Therefore, the RGD-conjugated BSANPs hold great potential as an effective drug delivery system to deliver therapeutic agents to pancreatic cancer.

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Cytotoxic effects of Gemcitabine-loaded liposomes in human anaplastic thyroid carcinoma cells

Abstract: Background: Identification of effective systemic antineoplastic drugs against anaplastic thyroid carcinomas has particularly important implications. In fact, the efficacy of the chemotherapeutic agents presently used in these tumours, is strongly limited by their low therapeutic index.

Cited by 85 publications

References 22 publications

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

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

Cytotoxic effects of a novel pyrazolopyrimidine derivative entrapped in liposomes in anaplastic thyroid cancer cells in vitro and in xenograft tumors in vivo

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

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