TY - JOUR
T1 - Preparation of spray dried amorphous solid dispersion of diosmin in soluplus with improved hepato-renoprotective activity
T2 - In vitro anti-oxidant and in-vivo safety studies
AU - Anwer, Md Khalid
AU - Ahmed, Mohammed Muqtader
AU - Alshetaili, Abdullah
AU - Almutairy, Bjad K.
AU - Alalaiwe, Ahmed
AU - Fatima, Farhat
AU - Ansari, Mohd Nazam
AU - Iqbal, Muzaffar
N1 - Publisher Copyright:
© 2020 Elsevier B.V.
PY - 2020/12
Y1 - 2020/12
N2 - In the current study, spray drying technique was utilized to prepare dissolution enhanced solid dispersion of a poorly soluble flavonoid, diosmin (DSM) with an excellent solubilizer, soluplus (SOL). Three formulae (F1–F3) of DSM-SOL solid dispersion powders were prepared in different ratio (1:0.5, 1:1 and 1:2, w/w) with a range of particle size (1.4–2.8 μm), PDI (0.257–0.349), ZP (−11.1 to −12.5 mV), content (67–82%) and yield (44–73%). Based on particle characterization, DSC, FTIR, PXRD, SEM and in-vitro studies, the spray dried solid dispersion (F3) formulae was optimized. The optimized formulae (F3) was additionally assessed for its in-vitro antioxidant activity and in-vivo protective effects against thioacetamide (TAA)-induced kidney and liver damage in rats. Results clearly indicate that pure DSM and F3 formulae significantly protected the renal and hepatic damage caused by TAA toxin. In addition, F3 formulae was found more protective than DSM as indicated by histopathological, and biochemical findings.
AB - In the current study, spray drying technique was utilized to prepare dissolution enhanced solid dispersion of a poorly soluble flavonoid, diosmin (DSM) with an excellent solubilizer, soluplus (SOL). Three formulae (F1–F3) of DSM-SOL solid dispersion powders were prepared in different ratio (1:0.5, 1:1 and 1:2, w/w) with a range of particle size (1.4–2.8 μm), PDI (0.257–0.349), ZP (−11.1 to −12.5 mV), content (67–82%) and yield (44–73%). Based on particle characterization, DSC, FTIR, PXRD, SEM and in-vitro studies, the spray dried solid dispersion (F3) formulae was optimized. The optimized formulae (F3) was additionally assessed for its in-vitro antioxidant activity and in-vivo protective effects against thioacetamide (TAA)-induced kidney and liver damage in rats. Results clearly indicate that pure DSM and F3 formulae significantly protected the renal and hepatic damage caused by TAA toxin. In addition, F3 formulae was found more protective than DSM as indicated by histopathological, and biochemical findings.
KW - Disomin
KW - Solid dispersion
KW - Solubilizer
KW - Soluplus
KW - Spray drying
UR - http://www.scopus.com/inward/record.url?scp=85091231778&partnerID=8YFLogxK
U2 - 10.1016/j.jddst.2020.102101
DO - 10.1016/j.jddst.2020.102101
M3 - Article
AN - SCOPUS:85091231778
SN - 1773-2247
VL - 60
JO - Journal of Drug Delivery Science and Technology
JF - Journal of Drug Delivery Science and Technology
M1 - 102101
ER -