ISSN: 2578-4803
Enhanced Intestinal Permeability of Silymarin by Natural Products as Bioenhancers - Assessment by Ex-Vivo Non-Everted Rat Gut Sac Study
Background: Silymarin, a widely used hepatoprotective drug, exhibits low oral bioavailability mainly because of poor water solubility, poor absorption, rapid metabolism and ultimately poor oral bioavailability of silymarin. Objective: Therefore, the present study was aimed to investigate the effects of Piperine, Fulvic acid and Lysergol as bioenhancers on the intestinal absorption of silymarin. Method: Non-everted sacs of rat small intestines were incubated in tyrode buffer solution which contained Silymarin in the absence or presence of various bioenhancers viz. Piperine, Fulvic acid and Lysergol alone and in combinations with each other in different concentrations. Result: It was found that Silymarin alone had apparent permeability coefficient Papp x 10-6 cm/s value of 1.63 and human fraction absorbed Fa (%) value of 21% as compared to which the highest values Papp x 10-6 cm/s 7.01 and Fa (%) > 100% were found to be for Silymarin- Fulvic acid (1:1) mixture + Piperine (10%). The absorption transport of Silymarin was significantly enhanced in the presence of Piperine and Fulvic acid, suggesting that the Piperine acted as hepatic and intestinal glucoronidation inhibitor of Silymarin and Fulvic acid increased the water solubility of Silymarin and aided in the transport of Silymarin across the intestinal epithelial cells. However, the addition of Lysergol at various concentrations (1%, 5% and 10%) had no significant effect on Silymarin transport. Conclusion: The results of the study suggest that the use of such effective bioenhancers in Silymarin formulations may enhance the oral absorption and hence the oral bioavailability of Silymarin.
Keywords:
Silymarin; Piperine; Fulvic acid; Lysergol; Permeability; Bioavailability; Solubility
