Sucrose acetate isobutyrate (SAIB) and glyceryl monooleate (GMO) hybrid nanoparticles for bioavailability enhancement of rivaroxaban : an optimization study

This study aims to improve the RXB bioavailability using hybrid nanoparticles. A modified melt dispersion technique created different formulas with varying GMO-SAIB: RXB and GMO: SAIB ratios, with fixed GMO-SAIB: poloxamer 407 ratios. The PS, PDI, ZP, and EE were measured to determine the optimal formula, which was selected using Design-Expert™ software. The optimized formula was lyophilized and tested for PS, PDI, ZP, and EE. The chosen lyophilized formula (L4) was characterized using FTIR, DSC, PXRD, dissolution studies, and pharmacokinetics studies. The study found correlations between variables and identified how GMO-SAIB concentration affects drug encapsulation. The dissolution parameters were calculated, including % Q5 and % DE). The % Q5 values were 68.4 ± 1.7% and 89.7 ± 3.6% for Xarelto and L4 tablets, respectively. The % DE values were 89.7 ± 0.4% and 97.5 ± 2.1% for Xarelto and L4 tablets, respectively. The AUC values were 2117.0 ng.h/mL (±77.3) and 3919.4 ng.h/mL (±134.8) for Xarelto and L4 tablets, respectively. The Cmax values were 241.3 ng/mL (±21.0) and 521.5 ng/mL (±91.5) for Xarelto and L4 tablets, respectively. In conclusion, the study found that using GMO-SAIB as co-formers effectively enhanced the bioavailability of RXB. The authors recommend using the hybrid nanoparticles technique and suggest further research to enhance its effectiveness for drug delivery.

Medienart:

E-Artikel

Erscheinungsjahr:

2023

Erschienen:

2023

Enthalten in:

Zur Gesamtaufnahme - volume:28

Enthalten in:

Pharmaceutical development and technology - 28(2023), 10 vom: 23. Dez., Seite 928-938

Sprache:

Englisch

Beteiligte Personen:

Al-Shoubki, Adam A [VerfasserIn]
Teaima, Mahmoud H [VerfasserIn]
Abdelmonem, Rehab [VerfasserIn]
El-Nabarawi, Mohamed A [VerfasserIn]
Elhabal, Sammar Fathy [VerfasserIn]

Links:

Volltext

Themen:

57-50-1
9NDF7JZ4M3
Bioavailability enhancement
C4YAD5F5G6
Glyceryl monooleate
H5KI1C3YTV
Journal Article
Monoolein
Nanonization
Rivaroxaban
Sucrose
Sucrose acetate isobutyrate

Anmerkungen:

Date Completed 20.12.2023

Date Revised 20.12.2023

published: Print-Electronic

Citation Status MEDLINE

doi:

10.1080/10837450.2023.2274944

funding:

Förderinstitution / Projekttitel:

PPN (Katalog-ID):

NLM363625291