TY - JOUR
T1 - Novel nano-encapsulation of probucol in microgels
T2 - scanning electron micrograph characterizations, buoyancy profiling, and antioxidant assay analyses
AU - Mooranian, Armin
AU - Zamani, Nassim
AU - Mikov, Momir
AU - Goločorbin-Kon, Svetlana
AU - Stojanovic, Goran
AU - Arfuso, Frank
AU - Al-Salami, Hani
N1 - Funding Information:
H. Al-Salami has been and is currently receiving funding from Beijing Nat-Med Biotechnology Co., Ltd. The authors would like to acknowledge the Australian Postgraduate Award (APA) and Curtin Research Scholarship (CRS). The authors also acknowledge the Curtin-seeding grant for the support and also acknowledge the use of laboratory equipment, scientific and technical assistance of Microscopy and Microanalysis Facility at Curtin University which has been partially funded by the University, State and Commonwealth Governments. The work is partially supported by the European Union Horizon 2020 MEDLEM research project and innovation program under the Marie Skłodowska-Curie Grant Agreement No 690876H.The NIT-1 cells were a generous donation from Professor Grant Morahan at the University of Western Australia.
Publisher Copyright:
© 2018, © 2018 Informa UK Limited, trading as Taylor & Francis Group.
PY - 2018/11/12
Y1 - 2018/11/12
N2 - Smart polymers such as Eudragit (ED) have shown potential applications in oral drug delivery and targeted release. Probucol (PB) is a lipophilic drug used for hypercholesterolemia and possesses desirable antidiabetic effects such as antioxidant and cell protective effects. PB is highly hydrophobic and has poor bioavailability with significant inter- and intra-patient absorption, limiting its clinical applications in diabetes. This study aimed to design and analyse new PB-ED formulations with or without the absorption-enhancer chenodeoxycholic acid (CDCA). Sodium alginate-based microcapsules containing three different ED polymers (NM30D, RL30D and RS30D) were investigated with or without CDCA via scanning electron microscopy, energy dispersive X-ray spectroscopy (EDXR), confocal microscopy, osmotic stability, mechanical properties, buoyancy, release profiles (pH: 7.4), thermal stability and antioxidant effects. The effects of microcapsules on pancreatic β-cell survival, function, inflammatory profile and PB cellular uptake were analysed. All microcapsules showed uniform morphology and surface topography with CDCA being distributed evenly throughout the microcapsules. Osmotic stability was significantly improved in PB-NM30D and PB-RL30D microcapsules (p
AB - Smart polymers such as Eudragit (ED) have shown potential applications in oral drug delivery and targeted release. Probucol (PB) is a lipophilic drug used for hypercholesterolemia and possesses desirable antidiabetic effects such as antioxidant and cell protective effects. PB is highly hydrophobic and has poor bioavailability with significant inter- and intra-patient absorption, limiting its clinical applications in diabetes. This study aimed to design and analyse new PB-ED formulations with or without the absorption-enhancer chenodeoxycholic acid (CDCA). Sodium alginate-based microcapsules containing three different ED polymers (NM30D, RL30D and RS30D) were investigated with or without CDCA via scanning electron microscopy, energy dispersive X-ray spectroscopy (EDXR), confocal microscopy, osmotic stability, mechanical properties, buoyancy, release profiles (pH: 7.4), thermal stability and antioxidant effects. The effects of microcapsules on pancreatic β-cell survival, function, inflammatory profile and PB cellular uptake were analysed. All microcapsules showed uniform morphology and surface topography with CDCA being distributed evenly throughout the microcapsules. Osmotic stability was significantly improved in PB-NM30D and PB-RL30D microcapsules (p
KW - chenodeoxycholic acid
KW - diabetes
KW - microencapsulation
KW - oxidative stress
KW - Probucol
KW - topographic analysis
UR - http://www.scopus.com/inward/record.url?scp=85053915902&partnerID=8YFLogxK
U2 - 10.1080/21691401.2018.1511571
DO - 10.1080/21691401.2018.1511571
M3 - Article
C2 - 30260253
AN - SCOPUS:85053915902
SN - 2169-1401
VL - 46
SP - S741-S747
JO - Artificial Cells, Nanomedicine and Biotechnology
JF - Artificial Cells, Nanomedicine and Biotechnology
IS - sup3
ER -