| Effect of Phospholipid-Based Formulations of Boswellia serrata Extract on the Solubility, Permeability, and Absorption of the Individual Boswellic Acid Constituents Present. | |
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MedLine Citation:
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PMID: 23013292 Owner: NLM Status: Publisher |
Abstract/OtherAbstract:
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Boswellia serrata gum resin extracts are used widely for the treatment of inflammatory diseases. However, very low concentrations in the plasma and brain were observed for the boswellic acids (1-6, the active constituents of B. serrata). The present study investigated the effect of phospholipids alone and in combination with common co-surfactants (e.g., Tween 80, vitamin E-TPGS, pluronic f127) on the solubility of 1-6 in physiologically relevant media and on the permeability in the Caco-2 cell model. Because of the high lipophilicity of 1-6, the permeability experiments were adapted to physiological conditions using modified fasted state simulated intestinal fluid as apical (donor) medium and 4% bovine serum albumin in the basolateral (receiver) compartment. A formulation composed of extract/phospholipid/pluronic f127 (1:1:1 w/w/w) increased the solubility of 1-6 up to 54 times compared with the nonformulated extract and exhibited the highest mass net flux in the permeability tests. The oral administration of this formulation to rats (240 mg/kg) resulted in 26 and 14 times higher plasma levels for 11-keto-β-boswellic acid (1) and acetyl-11-keto-β-boswellic acid (2), respectively. In the brain, five times higher levels for 2 compared to the nonformulated extract were determined 8 h after oral administration. |
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Authors:
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Jan Hüsch; Kathleen Gerbeth; Gert Fricker; Constanze Setzer; Jürgen Zirkel; Herbert Rebmann; Manfred Schubert-Zsilavecz; Mona Abdel-Tawab |
Publication Detail:
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Type: JOURNAL ARTICLE Date: 2012-9-26 |
Journal Detail:
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Title: Journal of natural products Volume: - ISSN: 1520-6025 ISO Abbreviation: J. Nat. Prod. Publication Date: 2012 Sep |
Date Detail:
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Created Date: 2012-9-27 Completed Date: - Revised Date: - |
Medline Journal Info:
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Nlm Unique ID: 7906882 Medline TA: J Nat Prod Country: - |
Other Details:
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Languages: ENG Pagination: - Citation Subset: - |
Affiliation:
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Central Laboratory of German Pharmacists , Carl-Mannich-Straße 20, 65760 Eschborn, Germany. |
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From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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