Probucol release from novel multicompartmental microcapsules for the oral targeted delivery in type 2 diabetes.

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.

• Authors: 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
• Journal: AAPS PharmSciTech (AAPS PharmSciTech) Vol. 16 Issue 1 Pg. 45-52 (Feb 2015) ISSN: 1530-9932 [Electronic] United States
• PMID: 25168450 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• Anticholesteremic Agents
• Capsules
• Delayed-Action Preparations
• Probucol

Topics

• Administration, Oral
• Anticholesteremic Agents (administration & dosage, chemistry)
• Body Fluids (chemistry)
• Capsules (administration & dosage, chemical synthesis)
• Delayed-Action Preparations (administration & dosage, chemical synthesis)
• Diabetes Mellitus, Type 2 (drug therapy)
• Diffusion
• Drug Compounding (methods)
• Drug Stability
• Humans
• Hydrogen-Ion Concentration
• Probucol (administration & dosage, chemistry)
• Temperature