Novel nano-encapsulation of probucol in microgels: scanning electron micrograph characterizations, buoyancy profiling, and antioxidant assay analyses
MetadataShow full item record
© 2018, © 2018 Informa UK Limited, trading as Taylor & Francis Group. 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 ß-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 <.01 and p <.05, respectively), and PB-NM30D microcapsules displayed low buoyancy (p <.01). CDCA improved PB-NM30D effects on pancreatic ß-cell function and bioenergetics, which suggests potential application of PB-NM30D-CDCA in PB delivery and diabetes treatment.
Showing items related by title, author, creator and subject.
Primary Bile Acid Chenodeoxycholic Acid-Based Microcapsules to Examine ß-cell Survival and the Inflammatory ResponseMooranian, A.; Negrulj, R.; Al-Salami, Hani (2016)In past studies using hydrogel-polyelectrolyte matrix and different bile acid excipients, we microencapsulated pancreatic ß-cells using various methods, and the microcapsules were mechanically stable, displayed good ...
Novel chenodeoxycholic acid-sodium alginate matrix in the microencapsulation of the potential antidiabetic drug, probucol. An in vitro studyMooranian, A.; Negrulj, R.; Mikov, M.; Golocorbin-Kon, S.; Arfuso, Frank; Al-Salami, Hani (2015)Context: We previously designed, developed and characterized a novel microencapsulated formulation as a platform for the targeted delivery of Probucol (PB) in an animal model of Type 2 Diabetes. Objective: The objective ...
The role of the bile acid chenodeoxycholic acid in the targeted oral delivery of the anti-diabetic drug gliclazide, and its applications in type 1 diabetesMathavan, S.; Chen-Tan, N.; Arfuso, Frank; Al-Salami, H. (2015)Gliclazide (G) is used to treat type 2 diabetes (T2D), and also has anti-platelet, anti-radical, and anti-inflammatory effects. G has poor water solubility and high inter-individual variations in absorption, limiting its ...