title: Swelling, mechanical strength, and release properties of probucol microcapsules with and without a bile acid, and their potential oral delivery in diabetes.
abstract: We have demonstrated a permeation-enhancing effect of deoxycholic acid (DCA), the bile acid, in diabetic rats. In this study, we designed DCA-based microcapsules for the oral delivery of the antilipidemic drug probucol (PB), which has potential antidiabetic effects. We aimed to further characterize these microcapsules and examine their pH-dependent release properties, as well as the effects of DCA on their stability and mechanical strength at various pH and temperature values. Using the polymer sodium alginate (SA), we prepared PB-SA (control) and PB-DCA-SA (test) microcapsules. The microcapsules were examined for drug content, size, surface composition, release, Micro-CT cross-sectional imaging, stability, Zeta potential, mechanical strength, and swelling characteristics at different pH and temperature values. The microencapsulation efficiency and production yield were also examined. The addition of DCA resulted in microcapsules with a greater density and with reduced swelling at a pH of 7.8 and at temperatures of 25°C and 37°C (p < 0.01). The size, surface composition, production yield, and microencapsulation efficiency of the microcapsules remained similar after DCA addition. PB-SA microcapsules produced multiphasic PB release, while PB-DCA-SA microcapsules produced monophasic PB release, suggesting more controlled PB release in the presence of DCA. The PB-DCA-SA microcapsules showed good stability and a pH-sensitive uniphasic release pattern, which may suggest potential applications in the oral delivery of PB in diabetes.
authors: a Biotechnology and Drug Development Research Laboratory, School of Pharmacy, Curtin Health Innovation Research Institute, Biosciences Research Precinct, Curtin University , Perth , Western Australia , Australia.
authors: Rebecca
authors: R
authors: Negrulj
authors: a Biotechnology and Drug Development Research Laboratory, School of Pharmacy, Curtin Health Innovation Research Institute, Biosciences Research Precinct, Curtin University , Perth , Western Australia , Australia.
authors: Armin
authors: A
authors: Mooranian
authors: b Faculty of Science & Engineering, Curtin University , Perth , Western Australia , Australia.
authors: Nigel
authors: N
authors: Chen-Tan
authors: c School of Pharmacy, University of Otago , Dunedin , New Zealand.
authors: Hesham S
authors: HS
authors: Al-Sallami
authors: d Department of Pharmacology , Toxicology and Clinical Pharmacology, Faculty of Medicine, University of Novi Sad , Novi Sad , Serbia.|e Department of Pharmacy , Faculty of Medicine, University of Montenegro , Podgorica , Montenegro.
authors: Momir
authors: M
authors: Mikov
authors: d Department of Pharmacology , Toxicology and Clinical Pharmacology, Faculty of Medicine, University of Novi Sad , Novi Sad , Serbia.|e Department of Pharmacy , Faculty of Medicine, University of Montenegro , Podgorica , Montenegro.
authors: Svetlana
authors: S
authors: Golocorbin-Kon
authors: f Faculty of Medicine, University of Montreal , Montreal , Quebec , Canada.
authors: Marc
authors: M
authors: Fakhoury
authors: g School of Medicine and Pharmacology, Royal Perth Hospital, University of Western Australia , Perth , Western Australia , Australia.
authors: Gerald F
authors: GF
authors: Watts
authors: h Stem Cell and Cancer Biology Laboratory, School of Biomedical Sciences, Curtin Health Innovation Research Institute, Biosciences Research Precinct, Curtin University , Perth , Western Australia , Australia.
authors: Frank
authors: F
authors: Arfuso
authors: a Biotechnology and Drug Development Research Laboratory, School of Pharmacy, Curtin Health Innovation Research Institute, Biosciences Research Precinct, Curtin University , Perth , Western Australia , Australia.
authors: Hani
authors: H
authors: Al-Salami
mesh_terms: D000284:Administration, Oral; D000818:Animals; D002214:Capsules; D003921:Diabetes Mellitus, Experimental / Q000188:drug therapy*; D007004:Hypoglycemic Agents / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D011341:Probucol / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D051381:Rats
chemical_list: D002214:Capsules; D007004:Hypoglycemic Agents; D011341:Probucol
keywords: Micro-CT imaging; deoxycholic acid; microencapsulation; production yield; release characteristics