Preparation and characterization of rivaroxaban nanocrystals prepared by combination of wet ball milling and high pressure homogenization methods
Latin American Journal of Pharmacy, cilt.37, sa.12, ss.2482-2490, 2018 (SCI-Expanded, Scopus)
- Yayın Türü: Makale / Tam Makale
- Cilt numarası: 37 Sayı: 12
- Basım Tarihi: 2018
- Dergi Adı: Latin American Journal of Pharmacy
- Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus
- Sayfa Sayıları: ss.2482-2490
- Anahtar Kelimeler: Ball milling, High pressure homogenization, Nanocrystal/nanosuspension, Permeability, Rivaroxaban
- Ondokuz Mayıs Üniversitesi Adresli: Hayır
Özet
The objectives of this study were to develop rivaroxaban (RXB) nanocrystals by combination of wet ball milling and high-pressure homogenization, and to increase the solubility and dissolution rate of RXB. A new nanocrystal formulation was developed, and used to reduce particle size of RXB which is a Biopharmaceutics Classification System Class 2 drug. Particle size of RXB in nanosuspension formulation (551 nm) and nanocrystal formulation (1018 nm) was reduced significantly (p < 0.05) as compared to the particle size of RXB bulk. Dissolution rate of RXB nanocrystals (85% within 15 min) was much faster than that of RXB bulk (12% within 45 min). Also, permeability across Caco-2 cells was enhanced for RXB nanocrystals (10.18 × 10 –5 cm/s) in comparison to the RXB bulk (7.25 × 10 –5 cm/s; p < 0.05). Based on the results, it can be concluded that nanocrystal technology can be employed to improve the solubility and dissolution rate of RXB (hence permeability) with preserving its chemical structure.