期刊
JOURNAL OF THROMBOSIS AND THROMBOLYSIS
卷 49, 期 3, 页码 404-412出版社
SPRINGER
DOI: 10.1007/s11239-019-02022-5
关键词
Rivaroxaban; PLGA; Nanoparticles; Bioavailability; Food effect
资金
- Deanship of Scientific Research at Prince Sattam Bin Abdulaziz University [2019/03/10912]
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 (R)) were conducted on fasted and fed state rats. Compared to commercial tablet (XARELTO (R)), 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.
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