Bio-relevant media to assess drug permeability: sodium taurocholate and lecithin combination or crude bile?
Berginc, Katja (Author), Trontelj, Jurij (Author), Kristl, Albin (Author)

URLURL - Presentation file, Visit http://www.sciencedirect.com/science/article/pii/S0378517312002372?v=s5 This link opens in a new window

The assessment of in vivo drug absorption with in vitro permeability models demands the use of transport media with surface acting compounds. With the aim to establish their influence on in vitro permeability of 30 drugs through Caco-2 monolayers, cell vitality/integrity and micellar drug entrapment, taurocholate/lecithin (NaTC/Leci) and pig crude bile were applied. Drug permeabilities were correlated to fraction of drugs absorbed and appropriate NaTC/Leci and bile concentrations were proposed to simulate fasted/fed conditions in vitro (bile in the concentration range 1-5 v/v% or 0.2/0.05 mM NaTC/Leci for fasted; 10 v/v% bile or 3/0.75 mM NaTC/Leci for fed conditions) without detrimental effects on monolayer integrity/vitality (NaTC/Leci was more toxic than bile). Surfactants exerted different affinities for drugs; free drug concentration (cfree) of some was significantly lowered only by bile, while for the others NaTC/Leci and bile significantly diminished cfree. For some substances NaTC/Leci and bile significantly increased their permeabilities (i.e. more than 3-times) in spite of profound cfree decrease indicating the existence of an alternative absorption mechanism. Based on these data, the impact of bile on in vitro drug permeability and micellar drug entrapment cannot be adequately simulated by NaTC/Leci, because their effects on drug absorption differ.

Keywords:lecitin, žolč, permeabilnost, absorpcija in vivo
Work type:Not categorized (r6)
Tipology:1.01 - Original Scientific Article
Organization:FFA - Faculty of Pharmacy
Number of pages:str. 22-30
Numbering:Vol. 429, issues 1-2
ISSN on article:0378-5173
DOI:10.1016/j.ijpharm.2012.03.015 Link is opened in a new window
COBISS.SI-ID:3217265 Link is opened in a new window
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Record is a part of a journal

Title:International journal of pharmaceutics
Shortened title:Int. j. pharm.
COBISS.SI-ID:3087631 This link opens in a new window

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