Sustained release and enhanced oral bioavailability of rivaroxaban by PLGA nanoparticles with no food effect

Md Khalid Anwer; Muqtader Mohammad; Muzaffar Iqbal; Mohd Nazam Ansari; Essam Ezzeldin; Farhat Fatima; Saad M. Alshahrani; Mohammed F. Aldawsari; Ahmed Alalaiwe; Aiman A. Alzahrani; Abdullah M. Aldayel

doi:10.1007/s11239-019-02022-5

Sustained release and enhanced oral bioavailability of rivaroxaban by PLGA nanoparticles with no food effect

Md Khalid Anwer
, Muqtader Mohammad
, Muzaffar Iqbal
, Mohd Nazam Ansari
, Essam Ezzeldin
, Farhat Fatima
, Saad M. Alshahrani
, Mohammed F. Aldawsari
, Ahmed Alalaiwe
, Aiman A. Alzahrani
, Abdullah M. Aldayel

Research output: Contribution to journal › Article › peer-review

50 Scopus citations

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.

Original language	English
Pages (from-to)	404-412
Number of pages	9
Journal	Journal of Thrombosis and Thrombolysis
Volume	49
Issue number	3
DOIs	https://doi.org/10.1007/s11239-019-02022-5
State	Published - 1 Apr 2020

Keywords

Bioavailability
Food effect
Nanoparticles
PLGA
Rivaroxaban

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10.1007/s11239-019-02022-5

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Anwer, M. K., Mohammad, M., Iqbal, M., Ansari, M. N., Ezzeldin, E., Fatima, F., Alshahrani, S. M., Aldawsari, M. F., Alalaiwe, A., Alzahrani, A. A., & Aldayel, A. M. (2020). Sustained release and enhanced oral bioavailability of rivaroxaban by PLGA nanoparticles with no food effect. Journal of Thrombosis and Thrombolysis, 49(3), 404-412. https://doi.org/10.1007/s11239-019-02022-5

@article{d1ed30f55d5d4156bfea9152f0ee1184,

title = "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{\textregistered}) were conducted on fasted and fed state rats. Compared to commercial tablet (XARELTO{\textregistered}), 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.",

keywords = "Bioavailability, Food effect, Nanoparticles, PLGA, Rivaroxaban",

author = "Anwer, \{Md Khalid\} and Muqtader Mohammad and Muzaffar Iqbal and Ansari, \{Mohd Nazam\} and Essam Ezzeldin and Farhat Fatima and Alshahrani, \{Saad M.\} and Aldawsari, \{Mohammed F.\} and Ahmed Alalaiwe and Alzahrani, \{Aiman A.\} and Aldayel, \{Abdullah M.\}",

note = "Publisher Copyright: {\textcopyright} 2020, Springer Science+Business Media, LLC, part of Springer Nature.",

year = "2020",

month = apr,

day = "1",

doi = "10.1007/s11239-019-02022-5",

language = "English",

volume = "49",

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Anwer, MK , Mohammad, M, Iqbal, M, Ansari, MN, Ezzeldin, E, Fatima, F, Alshahrani, SM , Aldawsari, MF , Alalaiwe, A, Alzahrani, AA & Aldayel, AM 2020, 'Sustained release and enhanced oral bioavailability of rivaroxaban by PLGA nanoparticles with no food effect', Journal of Thrombosis and Thrombolysis, vol. 49, no. 3, pp. 404-412. https://doi.org/10.1007/s11239-019-02022-5

TY - JOUR

T1 - Sustained release and enhanced oral bioavailability of rivaroxaban by PLGA nanoparticles with no food effect

AU - Anwer, Md Khalid

AU - Mohammad, Muqtader

AU - Iqbal, Muzaffar

AU - Ansari, Mohd Nazam

AU - Ezzeldin, Essam

AU - Fatima, Farhat

AU - Alshahrani, Saad M.

AU - Aldawsari, Mohammed F.

AU - Alalaiwe, Ahmed

AU - Alzahrani, Aiman A.

AU - Aldayel, Abdullah M.

PY - 2020/4/1

Y1 - 2020/4/1

N2 - 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.

AB - 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.

KW - Bioavailability

KW - Food effect

KW - Nanoparticles

KW - PLGA

KW - Rivaroxaban

UR - https://www.scopus.com/pages/publications/85077559025

U2 - 10.1007/s11239-019-02022-5

DO - 10.1007/s11239-019-02022-5

M3 - Article

C2 - 31898270

AN - SCOPUS:85077559025

SN - 0929-5305

VL - 49

SP - 404

EP - 412

JO - Journal of Thrombosis and Thrombolysis

JF - Journal of Thrombosis and Thrombolysis

IS - 3

ER -

Sustained release and enhanced oral bioavailability of rivaroxaban by PLGA nanoparticles with no food effect

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Keywords

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