Sustained release and enhanced oral bioavailability of rivaroxaban by PLGA nanoparticles with no food effect
Abstract The purpose of the currents study was to enhance bioavailability of rivaroxaban (RXB) and reduce the food effect. RXB loaded PLGA nanoparticles (RXB-PLGA-NPs) were prepared by emulsion solvent evaporation method and optimized using central composite design (CDD). The optimized RXB-PLGA-NPs (F8) with composition, PLGA (125 mg), PVA (0.5%w/w) and RXB (20 mg) was found optimum with particle size (496 ± 8.5 nm), PDI (0.607), ZP (− 18.41 ± 3.14 mV), %EE (87.9 ± 8.6) and %DL (9.5 ± 1.6). The optimized NPs (F8) was further evaluated in vitro for DSC, FTIR, SEM and in vitro release studies. A comparative pharmacokinetic studies with commercial tablet (XARELTO®) were conducted on fasted and fed state rats. Compared to commercial tablet (XARELTO®), the RXB-PLGA-NPs (F8) exhibited a significant enhancement of bioavailability in both fasted and fed state. In addition, the bioavailability of RXB from NPs (F8) was found unaffected in the presence of food..
| Medienart: |
E-Artikel |
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| Erscheinungsjahr: |
2020 |
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| Erschienen: |
2020 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:49 |
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| Enthalten in: |
Journal of thrombosis and thrombolysis - 49(2020), 3 vom: 02. Jan., Seite 404-412 |
| Sprache: |
Englisch |
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| Beteiligte Personen: |
Anwer, Md. Khalid [VerfasserIn] |
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| Links: |
Volltext [lizenzpflichtig] |
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| BKL: | |
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| Themen: |
| doi: |
10.1007/s11239-019-02022-5 |
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| 520 | |a Abstract The purpose of the currents study was to enhance bioavailability of rivaroxaban (RXB) and reduce the food effect. RXB loaded PLGA nanoparticles (RXB-PLGA-NPs) were prepared by emulsion solvent evaporation method and optimized using central composite design (CDD). The optimized RXB-PLGA-NPs (F8) with composition, PLGA (125 mg), PVA (0.5%w/w) and RXB (20 mg) was found optimum with particle size (496 ± 8.5 nm), PDI (0.607), ZP (− 18.41 ± 3.14 mV), %EE (87.9 ± 8.6) and %DL (9.5 ± 1.6). The optimized NPs (F8) was further evaluated in vitro for DSC, FTIR, SEM and in vitro release studies. A comparative pharmacokinetic studies with commercial tablet (XARELTO®) were conducted on fasted and fed state rats. Compared to commercial tablet (XARELTO®), the RXB-PLGA-NPs (F8) exhibited a significant enhancement of bioavailability in both fasted and fed state. In addition, the bioavailability of RXB from NPs (F8) was found unaffected in the presence of food. | ||
| 650 | 4 | |a Rivaroxaban |7 (dpeaa)DE-He213 | |
| 650 | 4 | |a PLGA |7 (dpeaa)DE-He213 | |
| 650 | 4 | |a Nanoparticles |7 (dpeaa)DE-He213 | |
| 650 | 4 | |a Bioavailability |7 (dpeaa)DE-He213 | |
| 650 | 4 | |a Food effect |7 (dpeaa)DE-He213 | |
| 700 | 1 | |a Mohammad, Muqtader |e verfasserin |4 aut | |
| 700 | 1 | |a Iqbal, Muzaffar |e verfasserin |4 aut | |
| 700 | 1 | |a Ansari, Mohd Nazam |e verfasserin |4 aut | |
| 700 | 1 | |a Ezzeldin, Essam |e verfasserin |4 aut | |
| 700 | 1 | |a Fatima, Farhat |e verfasserin |4 aut | |
| 700 | 1 | |a Alshahrani, Saad M. |e verfasserin |4 aut | |
| 700 | 1 | |a Aldawsari, Mohammed F. |e verfasserin |4 aut | |
| 700 | 1 | |a Alalaiwe, Ahmed |e verfasserin |4 aut | |
| 700 | 1 | |a Alzahrani, Aiman A. |e verfasserin |4 aut | |
| 700 | 1 | |a Aldayel, Abdullah M. |e verfasserin |4 aut | |
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