Artikel ; Online: Antitumor activity of the bioreductive prodrug 3-(2-nitrophenyl) propionic acid-paclitaxel nanoparticles (NPPA-PTX NPs) on MDA-MB-231 cells: in vitro and in vivo.
International journal of nanomedicine
2018 Band 14, Seite(n) 195–204
Abstract: Background: 3-(2-Nitrophenyl) propionic acid-paclitaxel (NPPA-PTX) is a paclitaxel (PTX) bioreductive prodrug synthesized by our lab. We hypothesize that NPPA-PTX can self-assemble to form nanoparticles (NPs).: Materials and methods: In the present ... ...
Abstract | Background: 3-(2-Nitrophenyl) propionic acid-paclitaxel (NPPA-PTX) is a paclitaxel (PTX) bioreductive prodrug synthesized by our lab. We hypothesize that NPPA-PTX can self-assemble to form nanoparticles (NPs). Materials and methods: In the present research, the theoretical partition coefficient (XlogP) and Hansen solubility parameters of NPPA-PTX were calculated. NPPA-PTX nanoparticles prepared by NPPA-PTX and DSPE-PEG (NPPA-PTX:DSPE-PEG =1:0.1, w/w) (NPPA-PTX@PEG NPs) were prepared and characterized. The cellular uptake, in vitro antitumor activity, in vivo targeting effect, tumor distribution, in vivo antitumor activity, and safety of NPPA-PTX@PEG NPs were investigated. Results: Our results indicate that NPPA-PTX can self-assemble to form NPPA-PTX@PEG NPs. Both the cellular uptake and safety of NPPA-PTX@PEG NPs were higher than those of Taxol. NPPA-PTX@PEG NPs could target tumor tissues by a passive targeting effect. In tumor tissues, NPPA-PTX@PEG NPs could completely transform into active PTX. The in vivo antitumor activity of NPPA-PTX@PEG NPs was confirmed in MDA-MB-231 tumor-bearing nude mice. Conclusion: The bioreductive prodrug NPPA-PTX could self-assemble to form NPs. The safety and antitumor activity of NPPA-PTX@PEG were confirmed in our in vitro and in vivo experiments. The NPPA-PTX@PEG NPs developed in this study could offer a new way of preparing bioreductive prodrug, self-assembled NPs suitable for antitumor therapy. |
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Mesh-Begriff(e) | Animals ; Apoptosis/drug effects ; Breast Neoplasms/drug therapy ; Breast Neoplasms/pathology ; Cell Proliferation/drug effects ; Female ; Humans ; In Vitro Techniques ; Mice ; Mice, Inbred BALB C ; Mice, Inbred ICR ; Mice, Nude ; Nanoparticles/administration & dosage ; Paclitaxel/administration & dosage ; Paclitaxel/analogs & derivatives ; Paclitaxel/pharmacology ; Phenylpropionates/administration & dosage ; Phenylpropionates/pharmacology ; Prodrugs/administration & dosage ; Prodrugs/pharmacology ; Tumor Cells, Cultured ; Xenograft Model Antitumor Assays |
Chemische Substanzen | 3-(2-nitrophenyl)propionic acid-paclitaxel ; Phenylpropionates ; Prodrugs ; Paclitaxel (P88XT4IS4D) |
Sprache | Englisch |
Erscheinungsdatum | 2018-12-24 |
Erscheinungsland | New Zealand |
Dokumenttyp | Journal Article |
ZDB-ID | 2364941-0 |
ISSN | 1178-2013 ; 1176-9114 |
ISSN (online) | 1178-2013 |
ISSN | 1176-9114 |
DOI | 10.2147/IJN.S186556 |
Datenquelle | MEDical Literature Analysis and Retrieval System OnLINE |
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