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. 2011 Dec 14;16(12):10347-56.
doi: 10.3390/molecules161210347.

Preparation and evaluation of berberine alginate beads for stomach-specific delivery

Zhen-Hai Zhang  1 , Yong-Shun Sun, Hui Pang, Were L L Munyendo, Hui-Xia Lv, Sheng-Liang Zhu
Affiliations

Preparation and evaluation of berberine alginate beads for stomach-specific delivery

Zhen-Hai Zhang et al. Molecules. .

Abstract

The purpose of this research was to prepare floating calcium alginate beads of berberine for targeting the gastric mucosa and prolonging their gastric residence time. The floating beads were prepared by suspending octodecanol and berberine in sodium alginate (SA) solution. The suspension was then dripped into a solution of calcium chloride. The hydrophobic and low-density octodecanol enhanced the sustained-release properties and floating ability of the beads. The bead formulation was optimized for different weight ratios of octodecanol and SA and evaluated in terms of diameter, floating ability and drug loading, entrapment and release. In vitro release studies showed that the floating and sustained release time were effectively increased in gastric media by addition of octodecanol. In vivo studies with rats showed that a significant increase in gastric residence time of beads had been achieved.

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Conflict of interest statement

The authors declare no conflict of interest.

Figures

Figure 1
Figure 1
Calcium alginate beads prepared by the dripping technique (the four figures are not at the same ratio); (a) the free beads before dehydration (mean diameter = 2.44 mm); (b) the free beads after dehydration, (mean diameter = 0.85 mm); (c) the berberine beads before dehydration with 88.7% drug loading (mean diameter = 2.98 mm); (d) the berberine beads after dehydration with 88.7% drug loading (mean diameter = 2.07 mm).
Figure 2
Figure 2
Release profile from berbeine SA beads.
See this image and copyright information in PMC

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