TY - JOUR
T1 - Formulation, characterization, in vitro and in vivo evaluations of self-nanoemulsifying drug delivery system of luteolin
AU - Javed Ansari, Mohammad
AU - Alshetaili, Abdullah
AU - Aldayel, Ibrahim Abdulaziz
AU - Alablan, Faisal Mohammed
AU - Alsulays, Bader
AU - Alshahrani, Saad
AU - Alalaiwe, Ahmad
AU - Ansari, Mohd Nazam
AU - Ur Rehman, Najeeb
AU - Shakeel, Faiyaz
N1 - Publisher Copyright:
© 2020 The Author(s). Published by Informa UK Limited, trading as Taylor & Francis Group.
PY - 2020
Y1 - 2020
N2 - The purpose of this study was to develop a self-nanoemulsifying drug delivery system (SNEDDS) for the improvement of solubility and bioavailability of luteolin in order to enhance its therapeutic benefits. Formulations were prepared by spontaneous emulsification method which involved low energy mixing of appropriate amounts ofcastor oil, kolliphor & polyethylene glycol 200. The developed formulae were optimized and characterized for self-nanoemulsifying capacity, thermodynamic stability, size behaviour and solubility. The globule size of the optimized formula F1–A1:1 was 112 ± 15 nm, with narrow PDI (0.31 ± 0.09) and good zeta potential (−16.2 ± 3.2 mV). The optimized formula exhibited approximately 83, 17 and 3-fold enhancement in the solubility in vitro release and ex vivo permeation respectively. The luteolin SNEDD exhibited better antioxidant activity (DPPH scavenging activity) than ascorbic acid. Per cent inhibition in rat paw oedema by the SNEDDS formulation was statistically significant when compared with luteolin suspension at equivalent dose (P < 0.05).
AB - The purpose of this study was to develop a self-nanoemulsifying drug delivery system (SNEDDS) for the improvement of solubility and bioavailability of luteolin in order to enhance its therapeutic benefits. Formulations were prepared by spontaneous emulsification method which involved low energy mixing of appropriate amounts ofcastor oil, kolliphor & polyethylene glycol 200. The developed formulae were optimized and characterized for self-nanoemulsifying capacity, thermodynamic stability, size behaviour and solubility. The globule size of the optimized formula F1–A1:1 was 112 ± 15 nm, with narrow PDI (0.31 ± 0.09) and good zeta potential (−16.2 ± 3.2 mV). The optimized formula exhibited approximately 83, 17 and 3-fold enhancement in the solubility in vitro release and ex vivo permeation respectively. The luteolin SNEDD exhibited better antioxidant activity (DPPH scavenging activity) than ascorbic acid. Per cent inhibition in rat paw oedema by the SNEDDS formulation was statistically significant when compared with luteolin suspension at equivalent dose (P < 0.05).
KW - anti-inflammatory
KW - DPPH
KW - Luteolin
KW - permeation
KW - self-nanoemulsifying system
KW - solubility
UR - http://www.scopus.com/inward/record.url?scp=85112767790&partnerID=8YFLogxK
U2 - 10.1080/16583655.2020.1812269
DO - 10.1080/16583655.2020.1812269
M3 - Article
AN - SCOPUS:85112767790
SN - 1658-3655
VL - 14
SP - 1386
EP - 1401
JO - Journal of Taibah University for Science
JF - Journal of Taibah University for Science
IS - 1
ER -