AAPS PharmSciTech

, Volume 16, Issue 1, pp 45–52 | Cite as

Probucol Release from Novel Multicompartmental Microcapsules for the Oral Targeted Delivery in Type 2 Diabetes

  • Armin Mooranian
  • Rebecca Negrulj
  • Hesham S. Al-Sallami
  • Zhongxiang Fang
  • Momir Mikov
  • Svetlana Golocorbin-Kon
  • Marc Fakhoury
  • Gerald F. Watts
  • Vance Matthews
  • Frank Arfuso
  • Amanda Lambros
  • Hani Al-Salami
Research Article


In previous studies, we developed and characterised multicompartmental microcapsules as a platform for the targeted oral delivery of lipophilic drugs in type 2 diabetes (T2D). We also designed a new microencapsulated formulation of probucol-sodium alginate (PB-SA), with good structural properties and excipient compatibility. The aim of this study was to examine the stability and pH-dependent targeted release of the microcapsules at various pH values and different temperatures. Microencapsulation was carried out using a Büchi-based microencapsulating system developed in our laboratory. Using SA polymer, two formulations were prepared: empty SA microcapsules (SA, control) and loaded SA microcapsules (PB-SA, test), at a constant ratio (1:30), respectively. Microcapsules were examined for drug content, zeta potential, size, morphology and swelling characteristics and PB release characteristics at pH 1.5, 3, 6 and 7.8. The production yield and microencapsulation efficiency were also determined. PB-SA microcapsules had 2.6 ± 0.25% PB content, and zeta potential of −66 ± 1.6%, suggesting good stability. They showed spherical and uniform morphology and significantly higher swelling at pH 7.8 at both 25 and 37°C (p < 0.05). The microcapsules showed multiphasic release properties at pH 7.8. The production yield and microencapsulation efficiency were high (85 ± 5 and 92 ± 2%, respectively). The PB-SA microcapsules exhibited distal gastrointestinal tract targeted delivery with a multiphasic release pattern and with good stability and uniformity. However, the release of PB from the microcapsules was not controlled, suggesting uneven distribution of the drug within the microcapsules.


anti-inflammatory antioxidant artificial-cell microencapsulation diabetes mellitus probucol type 2 diabetes 



The authors acknowledge the CHIRI at Curtin University and the Curtin-seeding grant for the 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.

Conflict of Interest

The authors declare no conflict of interest.


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Copyright information

© American Association of Pharmaceutical Scientists 2014

Authors and Affiliations

  • Armin Mooranian
    • 1
  • Rebecca Negrulj
    • 1
  • Hesham S. Al-Sallami
    • 2
  • Zhongxiang Fang
    • 3
  • Momir Mikov
    • 4
    • 5
  • Svetlana Golocorbin-Kon
    • 4
    • 5
  • Marc Fakhoury
    • 6
  • Gerald F. Watts
    • 7
  • Vance Matthews
    • 8
  • Frank Arfuso
    • 9
  • Amanda Lambros
    • 10
  • Hani Al-Salami
    • 1
    • 11
  1. 1.Biotechnology and Drug Development Research Laboratory, School of Pharmacy, Curtin Health Innovation Research Institute, Biosciences Research PrecinctCurtin UniversityPerthAustralia
  2. 2.School of PharmacyUniversity of OtagoDunedinNew Zealand
  3. 3.School of Public HealthCurtin UniversityPerthAustralia
  4. 4.Department of Pharmacology, Toxicology and Clinical Pharmacology, Faculty of MedicineUniversity of Novi SadNovi SadSerbia
  5. 5.Department of Pharmacy, Faculty of MedicineUniversity of MontenegroPodgoricaMontenegro
  6. 6.Faculty of MedicineUniversity of MontrealMontrealCanada
  7. 7.School of Medicine and Pharmacology, Royal Perth HospitalUniversity of Western AustraliaPerthAustralia
  8. 8.Laboratory for Metabolic Dysfunction, UWA Centre for Medical ResearchHarry Perkins Institute of Medical ResearchNedlandsAustralia
  9. 9.School of Biomedical Science, Curtin Health Innovation Research Institute, Biosciences Research PrecinctCurtin UniversityPerthAustralia
  10. 10.Faculty of Health Sciences, School of Occupational Therapy and Social WorkCurtin UniversityPerthAustralia
  11. 11.School of PharmacyCurtin UniversityBentlyAustralia

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