TY - JOUR
T1 - Novel chenodeoxycholic acid-sodium alginate matrix in the microencapsulation of the potential antidiabetic drug, probucol. An in vitro study
AU - Mooranian, Armin
AU - Negrulj, Rebecca
AU - Mikov, Momir
AU - Golocorbin-Kon, Svetlana
AU - Arfuso, Frank
AU - Al-Salami, Hani
N1 - Funding Information:
The authors acknowledge the CHIRI and Pharmacology Technical Laboratory at Curtin University, and the Curtin-seeding grant for their support and also acknowledge the use of equipment, scientific and technical assistance of the Curtin University Electron Microscope Facility, which has been partially funded by the University, State and Commonwealth Governments.
Publisher Copyright:
© 2015 Informa UK Ltd. All rights reserved: reproduction in whole or part not permitted.
PY - 2015/8/18
Y1 - 2015/8/18
N2 - 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 of this study is to optimize this platform by incorporating Chenodeoxycholic acid (CDCA), a bile acid with good permeation-enhancing properties, and examine its effect in vitro. Using sodium alginate (SA), we prepared PB-SA (control) and PB-CDCA-SA (test) microcapsules. Results and discussion: CDCA resulted in better structural and surface characteristics, uniform morphology, and stable chemical and thermal profiles, while size and rheological parameters remained unchanged. PB-CDCA-SA microcapsules showed good excipients compatibilities, as evidenced by differential scanning calorimetry (DSC), Fourier transform infrared spectroscopy, scanning electron microscopy and energy dispersive X-ray spectroscopy studies. CDCA reduced microcapsule swelling at pH 7.8 at both 37 °C and 25 °C and improved PB-release. Conclusion: CDCA improved the characteristics and release properties of PB-microcapsules and may have potential in the targeted oral delivery of PB.
AB - 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 of this study is to optimize this platform by incorporating Chenodeoxycholic acid (CDCA), a bile acid with good permeation-enhancing properties, and examine its effect in vitro. Using sodium alginate (SA), we prepared PB-SA (control) and PB-CDCA-SA (test) microcapsules. Results and discussion: CDCA resulted in better structural and surface characteristics, uniform morphology, and stable chemical and thermal profiles, while size and rheological parameters remained unchanged. PB-CDCA-SA microcapsules showed good excipients compatibilities, as evidenced by differential scanning calorimetry (DSC), Fourier transform infrared spectroscopy, scanning electron microscopy and energy dispersive X-ray spectroscopy studies. CDCA reduced microcapsule swelling at pH 7.8 at both 37 °C and 25 °C and improved PB-release. Conclusion: CDCA improved the characteristics and release properties of PB-microcapsules and may have potential in the targeted oral delivery of PB.
KW - Bile acids
KW - Chenodeoxycholic acid
KW - Microencapsulation
KW - Probucol
KW - Type 2 diabetes mellitus
UR - http://www.scopus.com/inward/record.url?scp=84940906595&partnerID=8YFLogxK
U2 - 10.3109/02652048.2015.1065922
DO - 10.3109/02652048.2015.1065922
M3 - Article
C2 - 26190214
AN - SCOPUS:84940906595
SN - 0265-2048
VL - 32
SP - 589
EP - 597
JO - Journal of Microencapsulation
JF - Journal of Microencapsulation
IS - 6
ER -
