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• Munyendo, W
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Molecules 2011, 16(12), 10347-10356; doi:10.3390/molecules161210347

Article

Preparation and Evaluation of Berberine Alginate Beads for Stomach-Specific Delivery

Zhen-Hai Zhang ^1,† , Yong-Shun Sun ^2,† , Hui Pang ³ , Were L.L. Munyendo ⁴ , Hui-Xia Lv ^4,*  and Sheng-Liang Zhu ^2,*

¹ Jiangsu Province Academy of Traditional Chinese Medicine, No. 100 shizhijie, Nanjing 210028, China ² Yueyang Hospital of Integrated Traditional Chinese and Western Medicine, Shanghai University of Traditional Chinese Medicine, No. 110 ganhelu, Shanghai 200437, China ³ Jiangsu Institute for Food and Drug Control, No. 6 beijingxilu, Nanjing 210024, China ⁴ Department of Pharmaceutics, China Pharmaceutical University, No. 24 tongjiaxiang, Nanjing 210009, China ^† These authors contributed equally to this work.

* Authors to whom correspondence should be addressed.

Received: 10 November 2011; in revised form: 25 November 2011 / Accepted: 5 December 2011 / Published: 14 December 2011

(This article belongs to the Section Natural Products)

Download PDF Full-Text [254 KB, uploaded 14 December 2011 09:14 CET]

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.

Keywords: berberine; octodecanol; calcium alginate beads; buoyancy; gastric residence

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