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Biocompatible and biodegradable fibrinogen microspheres for tumor-targeted doxorubicin delivery.

Joo JY, Park GY, An SS - Int J Nanomedicine (2015)

Bottom Line: Doxorubicin (DOX), a chemotherapeutic agent, was covalently conjugated to Fbg, and the microspheres were prepared.In vitro cytotoxicity tests confirmed low cytotoxicity in normal cells and high antitumor effect toward cancer cells.Therefore, DOX-linker-Fbg microspheres could be a suitable drug carrier for safer and effective drug delivery.

View Article: PubMed Central - PubMed

Affiliation: Department of Bionano Technology, Gachon Medical Research Institute, Gachon University, Seongnam-si, Republic of Korea.

ABSTRACT
In the development of effective drug delivery carriers, many researchers have focused on the usage of nontoxic and biocompatible materials and surface modification with targeting molecules for tumor-specific drug delivery. Fibrinogen (Fbg), an abundant glycoprotein in plasma, could be a potential candidate for developing drug carriers because of its biocompatibility and tumor-targeting property via arginine-glycine-aspartate (RGD) peptide sequences. Doxorubicin (DOX), a chemotherapeutic agent, was covalently conjugated to Fbg, and the microspheres were prepared. Acid-labile and non-cleavable linkers were used for the conjugation of DOX to Fbg, resulting in an acid-triggered drug release under a mild acidic condition and a slow-controlled drug release, respectively. In vitro cytotoxicity tests confirmed low cytotoxicity in normal cells and high antitumor effect toward cancer cells. In addition, it was discovered that a longer linker could make the binding of cells to Fbg drug carriers easier. Therefore, DOX-linker-Fbg microspheres could be a suitable drug carrier for safer and effective drug delivery.

No MeSH data available.


Related in: MedlinePlus

Cell viability according to the treatment of DOX–linker–Fbg microspheres after 24 hours.Abbreviations: DOX, doxorubicin; Fbg, fibrinogen; L, linker.
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f7-ijn-10-101: Cell viability according to the treatment of DOX–linker–Fbg microspheres after 24 hours.Abbreviations: DOX, doxorubicin; Fbg, fibrinogen; L, linker.

Mentions: The cytotoxicity of the DOX–linker–Fbg microspheres was evaluated with NIH-3T3 as a normal fibroblast and SH-SY5Y as an abnormal tumor cell line by performing the celltiter-glo® luminescence assay (Figure 7). Free-DOX solution (0.39 µg/mL) was added to the cells, revealing 43.90% of NIH-3T3 cell viability and 21.23% of SH-SY5Y cell viability. Higher toxicity to normal cells and abnormal tumor cells was observed, without low specificity to the targeting of tumor cells, which demonstrates a potential side effect of DOX. However, when bare-Fbg microspheres were treated, slightly increased cell viability was measured in both cell lines, due to the cytocompatiblity of Fbg.


Biocompatible and biodegradable fibrinogen microspheres for tumor-targeted doxorubicin delivery.

Joo JY, Park GY, An SS - Int J Nanomedicine (2015)

Cell viability according to the treatment of DOX–linker–Fbg microspheres after 24 hours.Abbreviations: DOX, doxorubicin; Fbg, fibrinogen; L, linker.
© Copyright Policy
Related In: Results  -  Collection

License
Show All Figures
getmorefigures.php?uid=PMC4562758&req=5

f7-ijn-10-101: Cell viability according to the treatment of DOX–linker–Fbg microspheres after 24 hours.Abbreviations: DOX, doxorubicin; Fbg, fibrinogen; L, linker.
Mentions: The cytotoxicity of the DOX–linker–Fbg microspheres was evaluated with NIH-3T3 as a normal fibroblast and SH-SY5Y as an abnormal tumor cell line by performing the celltiter-glo® luminescence assay (Figure 7). Free-DOX solution (0.39 µg/mL) was added to the cells, revealing 43.90% of NIH-3T3 cell viability and 21.23% of SH-SY5Y cell viability. Higher toxicity to normal cells and abnormal tumor cells was observed, without low specificity to the targeting of tumor cells, which demonstrates a potential side effect of DOX. However, when bare-Fbg microspheres were treated, slightly increased cell viability was measured in both cell lines, due to the cytocompatiblity of Fbg.

Bottom Line: Doxorubicin (DOX), a chemotherapeutic agent, was covalently conjugated to Fbg, and the microspheres were prepared.In vitro cytotoxicity tests confirmed low cytotoxicity in normal cells and high antitumor effect toward cancer cells.Therefore, DOX-linker-Fbg microspheres could be a suitable drug carrier for safer and effective drug delivery.

View Article: PubMed Central - PubMed

Affiliation: Department of Bionano Technology, Gachon Medical Research Institute, Gachon University, Seongnam-si, Republic of Korea.

ABSTRACT
In the development of effective drug delivery carriers, many researchers have focused on the usage of nontoxic and biocompatible materials and surface modification with targeting molecules for tumor-specific drug delivery. Fibrinogen (Fbg), an abundant glycoprotein in plasma, could be a potential candidate for developing drug carriers because of its biocompatibility and tumor-targeting property via arginine-glycine-aspartate (RGD) peptide sequences. Doxorubicin (DOX), a chemotherapeutic agent, was covalently conjugated to Fbg, and the microspheres were prepared. Acid-labile and non-cleavable linkers were used for the conjugation of DOX to Fbg, resulting in an acid-triggered drug release under a mild acidic condition and a slow-controlled drug release, respectively. In vitro cytotoxicity tests confirmed low cytotoxicity in normal cells and high antitumor effect toward cancer cells. In addition, it was discovered that a longer linker could make the binding of cells to Fbg drug carriers easier. Therefore, DOX-linker-Fbg microspheres could be a suitable drug carrier for safer and effective drug delivery.

No MeSH data available.


Related in: MedlinePlus