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

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Abstract

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.

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Acknowledgments

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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Authors and Affiliations

  1. Biotechnology and Drug Development Research Laboratory, School of Pharmacy, Curtin Health Innovation Research Institute, Biosciences Research Precinct, Curtin University, Perth, WA, Australia

    Armin Mooranian, Rebecca Negrulj & Hani Al-Salami

  2. School of Pharmacy, University of Otago, Dunedin, New Zealand

    Hesham S. Al-Sallami

  3. School of Public Health, Curtin University, Perth, WA, Australia

    Zhongxiang Fang

  4. Department of Pharmacology, Toxicology and Clinical Pharmacology, Faculty of Medicine, University of Novi Sad, Novi Sad, Serbia

    Momir Mikov & Svetlana Golocorbin-Kon

  5. Department of Pharmacy, Faculty of Medicine, University of Montenegro, Podgorica, Montenegro

    Momir Mikov & Svetlana Golocorbin-Kon

  6. Faculty of Medicine, University of Montreal, Montreal, Quebec, Canada

    Marc Fakhoury

  7. School of Medicine and Pharmacology, Royal Perth Hospital, University of Western Australia, Perth, WA, Australia

    Gerald F. Watts

  8. Laboratory for Metabolic Dysfunction, UWA Centre for Medical Research, Harry Perkins Institute of Medical Research, Nedlands, WA, Australia

    Vance Matthews

  9. School of Biomedical Science, Curtin Health Innovation Research Institute, Biosciences Research Precinct, Curtin University, Perth, WA, Australia

    Frank Arfuso

  10. Faculty of Health Sciences, School of Occupational Therapy and Social Work, Curtin University, Perth, WA, Australia

    Amanda Lambros

  11. School of Pharmacy, Curtin University, Bently, WA, Australia

    Hani Al-Salami

Authors
  1. Armin Mooranian
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  2. Rebecca Negrulj
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  3. Hesham S. Al-Sallami
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  4. Zhongxiang Fang
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  5. Momir Mikov
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  6. Svetlana Golocorbin-Kon
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  7. Marc Fakhoury
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  8. Gerald F. Watts
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  9. Vance Matthews
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  10. Frank Arfuso
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  11. Amanda Lambros
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  12. Hani Al-Salami
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Corresponding author

Correspondence to Hani Al-Salami.

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Mooranian, A., Negrulj, R., Al-Sallami, H.S. et al. Probucol Release from Novel Multicompartmental Microcapsules for the Oral Targeted Delivery in Type 2 Diabetes. AAPS PharmSciTech 16, 45–52 (2015). https://doi.org/10.1208/s12249-014-0205-9

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  • DOI: https://doi.org/10.1208/s12249-014-0205-9

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