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DOI: 10.1055/s-0031-1273632
Intestinal Transport of Bacopaside X and Bacopasaponin C Isolated from Bacopa Monnieri – In situ and In vitro Approaches
Bacopa monnieri (L.) Pennell. (Scrophulariaceae) has been used for its memory enhancing properties and as a nerve tonic for the treatment of epilepsy and insanity in Ayurvedic medicine. In the Western world several commercial products are available claiming adaptogenic and cognitive enhancing effects. Presence of dammarane-type saponins (bacopasides) is considered to be responsible for the pharmacological properties of Bacopa monnieri. Bacopa monnieri is administered orally but nothing is known about intestinal absorption and transport properties of bacopasides. The present study was aimed to predict the intestinal absorption and transport of bacopaside X and bacopasaponin C utilizing Caco-2 cell monolayer and in situ intestinal perfusion models. Quantitation was performed by UPLC/MS method. In the Caco-2 cell model, bacopaside X exhibited bidirectional transport with a Papp value of 4.7×10-6 cm/s and 6.1×10-6 cm/s in the absorptive and secretory directions indicating its passive diffusion. The transport of bacopaside X was two fold higher than that of low permeable marker atenolol in both directions. However no transport was observed for bacopasaponin C. In the perfused rat intestinal model, absorption of bacopaside X and bacopasaponin C was low with a permeability coefficient (Plumen) in the range of 3.0–8.1×10-6 cm/s and the results were comparable to atenolol (4.0–6.0×10-6 cm/s). These results from in situ intestinal perfusion and in vitro Caco-2 model indicated a low absorption of bacopaside X and bacopasaponin C across intestinal epithelium.