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Effect of Phospholipid-Based Formulations of Boswellia serrata Extract on the Solubility, Permeability, and Absorption of the Individual Boswellic Acid Constituents Present.
MedLine Citation:
PMID:  23013292     Owner:  NLM     Status:  Publisher    
Abstract/OtherAbstract:
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.
Authors:
Jan Hüsch; Kathleen Gerbeth; Gert Fricker; Constanze Setzer; Jürgen Zirkel; Herbert Rebmann; Manfred Schubert-Zsilavecz; Mona Abdel-Tawab
Publication Detail:
Type:  JOURNAL ARTICLE     Date:  2012-9-26
Journal Detail:
Title:  Journal of natural products     Volume:  -     ISSN:  1520-6025     ISO Abbreviation:  J. Nat. Prod.     Publication Date:  2012 Sep 
Date Detail:
Created Date:  2012-9-27     Completed Date:  -     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  7906882     Medline TA:  J Nat Prod     Country:  -    
Other Details:
Languages:  ENG     Pagination:  -     Citation Subset:  -    
Affiliation:
Central Laboratory of German Pharmacists , Carl-Mannich-Straße 20, 65760 Eschborn, Germany.
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