TY - JOUR
T1 - Impact of carrier hydrophilicity on solid self nano-emulsifying drug delivery system and self nano-emulsifying granule system
AU - Kim, Jung Suk
AU - Din, Fakhar ud
AU - Cho, Hyuk Jun
AU - Choi, Yoo Jin
AU - Woo, Mi Ran
AU - Cheon, Seunghyun
AU - Ji, Sang Hun
AU - Park, Seonghyeon
AU - Youn, Yu Seok
AU - Oh, Kyung Taek
AU - Lim, Soo Jeong
AU - Jin, Sung Giu
AU - Choi, Han Gon
N1 - Publisher Copyright:
© 2023 Elsevier B.V.
PY - 2023/12/15
Y1 - 2023/12/15
N2 - The purpose of this study was to investigate the impact of carrier hydrophilicity on solid self nano-emulsifying drug delivery system (SNEDDS) and self nano-emulsifying granule system (SEGS). The mesoporous calcium silicate (Ca-silicate) and hydroxypropyl-β-cyclodextrin (HP-β-CD) were utilised as hydrophobic carrier and hydrophilic carrier, respectively. The liquid SNEDDS formulation, composed of Tween80/Kollipohr EL/corn oil (35/50/15%) with 31% (w/w) dexibuprofen, was spray-dried and fluid-bed granulated together with Avicel using Ca-silicate or HP- β-CD as a solid carrier, producing four different solid SNEDDS and SEGS formulations. Unlike the Ca-silicate-based systems, spherical shape and aggregated particles were shown in HP-β-CD-based solid SNEDDS and SEGS, respectively. Molecular interaction was detected between Ca-silicate and the drug; though, none was shown between HP-β-CD and the drug. Each system prepared with either carrier gave no significant differences in micromeritic properties, crystallinity, droplet morphology, size, dissolution and oral bioavailability in rats. However, the HP-β-CD-based system more significantly improved the drug solubility than did the Ca-silicate-based system. Therefore, both carriers hardly affected the properties of both solid SNEDDS and SEGS; though, there were differences in the aspect of appearance, molecular interaction and solubility.
AB - The purpose of this study was to investigate the impact of carrier hydrophilicity on solid self nano-emulsifying drug delivery system (SNEDDS) and self nano-emulsifying granule system (SEGS). The mesoporous calcium silicate (Ca-silicate) and hydroxypropyl-β-cyclodextrin (HP-β-CD) were utilised as hydrophobic carrier and hydrophilic carrier, respectively. The liquid SNEDDS formulation, composed of Tween80/Kollipohr EL/corn oil (35/50/15%) with 31% (w/w) dexibuprofen, was spray-dried and fluid-bed granulated together with Avicel using Ca-silicate or HP- β-CD as a solid carrier, producing four different solid SNEDDS and SEGS formulations. Unlike the Ca-silicate-based systems, spherical shape and aggregated particles were shown in HP-β-CD-based solid SNEDDS and SEGS, respectively. Molecular interaction was detected between Ca-silicate and the drug; though, none was shown between HP-β-CD and the drug. Each system prepared with either carrier gave no significant differences in micromeritic properties, crystallinity, droplet morphology, size, dissolution and oral bioavailability in rats. However, the HP-β-CD-based system more significantly improved the drug solubility than did the Ca-silicate-based system. Therefore, both carriers hardly affected the properties of both solid SNEDDS and SEGS; though, there were differences in the aspect of appearance, molecular interaction and solubility.
KW - Crystallinity
KW - Hydroxypropyl-β-cyclodextrin
KW - Micromeritic property
KW - Oral bioavailability
KW - Self nano-emulsifying granule system
KW - Solid self nano-emulsifying drug delivery system
UR - https://www.scopus.com/pages/publications/85176098404
U2 - 10.1016/j.ijpharm.2023.123578
DO - 10.1016/j.ijpharm.2023.123578
M3 - Article
C2 - 37931729
AN - SCOPUS:85176098404
SN - 0378-5173
VL - 648
JO - International Journal of Pharmaceutics
JF - International Journal of Pharmaceutics
M1 - 123578
ER -