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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.

journal_name

AAPS PharmSciTech

journal_title

AAPS PharmSciTech

authors

Mooranian A,Negrulj R,Al-Sallami HS,Fang Z,Mikov M,Golocorbin-Kon S,Fakhoury M,Watts GF,Matthews V,Arfuso F,Lambros A,Al-Salami H

doi

10.1208/s12249-014-0205-9

subject

Has Abstract

pub_date

2015-02-01 00:00:00

pages

45-52

issue

1

issn

1530-9932

journal_volume

16

pub_type

杂志文章

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