Microencapsulation as a novel delivery method for the potential antidiabetic drug, Probucol

Drug Des Devel Ther. 2014 Sep 9:8:1221-30. doi: 10.2147/DDDT.S67349. eCollection 2014.

Abstract

Introduction: In previous studies, we successfully designed complex multicompartmental microcapsules as a platform for the oral targeted delivery of lipophilic drugs in type 2 diabetes (T2D). Probucol (PB) is an antihyperlipidemic and antioxidant drug with the potential to show benefits in T2D. We aimed to create a novel microencapsulated formulation of PB and to examine the shape, size, and chemical, thermal, and rheological properties of these microcapsules in vitro.

Method: Microencapsulation was carried out using the Büchi-based microencapsulating system developed in our laboratory. Using the polymer, sodium alginate (SA), empty (control, SA) and loaded (test, PB-SA) microcapsules were prepared at a constant ratio (1:30). Complete characterizations of microcapsules, in terms of morphology, thermal profiles, dispersity, and spectral studies, were carried out in triplicate.

Results: PB-SA microcapsules displayed uniform and homogeneous characteristics with an average diameter of 1 mm. The microcapsules exhibited pseudoplastic-thixotropic characteristics and showed no chemical interactions between the ingredients. These data were further supported by differential scanning calorimetric analysis and Fourier transform infrared spectral studies, suggesting microcapsule stability.

Conclusion: The new PB-SA microcapsules have good structural properties and may be suitable for the oral delivery of PB in T2D. Further studies are required to examine the clinical efficacy and safety of PB in T2D.

Keywords: Probucol; anti-inflammatory; antioxidant; artificial cell microencapsulation; diabetes.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Administration, Oral
  • Alginates / administration & dosage
  • Alginates / chemistry
  • Diabetes Mellitus, Type 2 / drug therapy*
  • Drug Compounding
  • Drug Delivery Systems*
  • Glucuronic Acid / administration & dosage
  • Glucuronic Acid / chemistry
  • Hexuronic Acids / administration & dosage
  • Hexuronic Acids / chemistry
  • Hypoglycemic Agents / administration & dosage
  • Hypoglycemic Agents / chemistry
  • Hypoglycemic Agents / therapeutic use*
  • Particle Size
  • Probucol / administration & dosage
  • Probucol / chemistry
  • Probucol / therapeutic use*
  • Surface Properties

Substances

  • Alginates
  • Hexuronic Acids
  • Hypoglycemic Agents
  • Glucuronic Acid
  • Probucol